Any feedback?
Information on EC 3.4.14.5 - dipeptidyl-peptidase IV and Organism(s) Rattus norvegicus and UniProt Accession P14740
for references in articles please use BRENDA:EC3.4.14.5Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
3.4.14.5 dipeptidyl-peptidase IVSpecify your search results
Word Map
- 3.4.14.5
- mellitus
- glp-1
- peptide-1
- agonist
- cardiovascular
- sitagliptin
- metformin
-
antidiabetic
- incretins
-
glycemic
- sulfonylurea
- hypoglycemia
- vildagliptin
-
monotherapy
- hemoglobin
-
placebo
- pancreatic
-
glucose-lowering
-
glucose-dependent
-
sodium-glucose
- thiazolidinediones
-
insulinotropic
-
postprandial
-
glycated
-
incretin-based
- gip
- liraglutide
-
add-on
-
double-blind
- beta-cell
-
cotransporter
-
antihyperglycemic
-
exenatide
-
excursion
-
open-label
-
placebo-controlled
- pioglitazone
-
sulphonylureas
- pemphigoid
-
long-acting
-
bullous
- exendin-4
- mers-cov
-
real-world
- biguanides
-
once-daily
- medicine
-
macrovascular
-
once-weekly
- drug development
- veterinary medicine
- analysis
- pharmacology
- glargine
- food industry
-
enteroendocrine
- diagnostics
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Reaction Schemes
release of an N-terminal dipeptide, Xaa-Yaa-/-Zaa-, from a polypeptide, preferentially when Yaa is Pro, provided Zaa is neither Pro nor hydroxyproline
Synonyms
dpp-4, dipeptidyl peptidase-4, dpp-iv, dipeptidyl peptidase iv, dpp iv, dppiv, dipeptidyl peptidase 4, dipeptidyl peptidase-iv, dp iv, dipeptidylpeptidase iv, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
CD26
ACT3
-
-
-
-
ADABP
-
-
-
-
Adenosine deaminase complexing protein
-
-
-
-
amino acyl-prolyl dipeptidyl aminopeptidase
-
-
-
-
aminopeptidase, glycylproline
-
-
-
-
Bile canaliculus domain-specific membrane glycoprotein
-
-
-
-
dipeptidyl aminopeptidase IV
-
-
-
-
dipeptidyl peptidase IV
-
-
dipeptidyl-aminopeptidase IV
-
-
-
-
dipeptidyl-peptidase IV (CD26)
-
-
-
-
dipeptidyl-peptide hydrolase
-
-
-
-
DPP IV/CD26
-
-
-
-
DPP-4
-
-
DPP-IV
-
-
Gly-Pro-naphthylamidase
-
-
-
-
glycoprotein GP110
-
-
-
-
glycylproline aminopeptidase
-
-
-
-
glycylproline-dipeptidyl-aminopeptidase
-
-
-
-
glycylprolyl aminopeptidase
-
-
-
-
glycylprolyl dipeptidylaminopeptidase
-
-
-
-
GP110 glycoprotein
-
-
-
-
leukocyte antigen CD26
-
-
-
-
lymphocyte, antigen CD26
-
-
-
-
Pep X
-
-
-
-
peptidase, dipeptidyl, IV
-
-
-
-
postproline dipeptidyl aminopeptidase IV
-
-
-
-
T cell triggering molecule Tp103
-
-
-
-
T-cell activation antigen CD26
-
-
-
-
THAM
-
-
-
-
Thymocyte-activating molecule
-
-
-
-
TP103
-
-
-
-
WC10
-
-
-
-
X-PDAP
-
-
-
-
X-prolyl dipeptidyl aminopeptidase
-
-
-
-
Xaa-Pro-dipeptidyl-aminopeptidase
-
-
-
-
CD26
dipeptidyl-peptidase IV is identical with the adenosine deaminase binding protein CD26 on lymphocytes
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
release of an N-terminal dipeptide, Xaa-Yaa-/-Zaa-, from a polypeptide, preferentially when Yaa is Pro, provided Zaa is neither Pro nor hydroxyproline
cleaves dipeptides containing proline or alanine or one of several other amino acids at the penultimate position from the amino termini of substrates, contains a Ser-His-Asp catalytic triad, active site structure, the Glu-Glu motif is necessary for amino dipeptide selection
-
CAS REGISTRY NUMBER
COMMENTARY
54249-88-6
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Gly-L-Pro-4-methoxy-beta-naphthylamide + H2O
Gly-L-Pro + 4-methoxy-beta-naphthylamine
-
-
-
?
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly
Arg-Pro + Lys-Pro-Gln-Gln-Phe-Phe-Gly
-
-
-
-
?
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2 + H2O
Arg-Pro + Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2
-
-
-
-
?
Gly-hydroxyproline-4-nitroanilide + H2O
Gly-hydroxyproline + 4-nitroaniline
-
-
-
-
?
Gly-L-Pro-4-nitroanilide + H2O
Gly-L-Pro + 4-nitroaniline
-
-
-
-
?
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
Gly-L-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
Gly-Pro-4-methoxy-2-naphthylamide + H2O
Gly-Pro + 4-methoxy-2-naphthylamine
-
-
-
-
?
Gly-Pro-4-methylcoumarin 7-amide + H2O
Gly-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
Gly-Pro-4-methylcoumaryl-7-amide + H2O
Gly-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
Gly-Pro-7-amido-4-methylcoumarin + H2O
Gly-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
H-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
H-Ala-L-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
L-Ala-L-Pro + 7-amino-4-methylcoumarin
-
-
-
-
?
peptide YY + H2O
peptide YY fragment 3-36
-
high affinity substrate of DPP-IV
-
-
?
beta-casomorphin + H2O
?
-
beta-casomorphin from human, i.e. Tyr-Pro-Phe-Val-Glu-Pro-Ileu
-
-
?
beta-casomorphin + H2O
?
-
beta-casomorphin from bovine, i.e. Tyr-Pro-Phe-Val-Glu-Pro-Ile
-
-
?
Gly-Pro-2-naphthylamide + H2O
Gly-Pro + 2-naphthylamine
-
L-Gly-Pro-2-naphthylamide
-
-
?
Gly-Pro-4-nitroanilide + H2O
Gly-Pro + 4-nitroaniline
-
-
-
-
?
additional information
?
-
-
peptides with proline penultimate to the amino terminus are more favored substrates while those substrates having Leu at both the penultimate position and amino terminus Leu-Leu
-
-
?
additional information
?
-
-
LVV-hemorphin-7 and LVV-hemorphin-6 are no substrates for the enzyme
-
?
additional information
?
-
-
obligatory role of the enzyme in renal handling of proline- and hydroxyproline-containing peptides
-
-
?
additional information
?
-
-
binding of dipeptidyl peptidase IV to fibronectin may play a role in interaction of hepatocytes with extracellular matrix in vivo and possibly in matrix assembly
-
-
?
additional information
?
-
-
enzyme is important for metabolic regulation
-
?
additional information
?
-
-
hemorphins may represent endogenous regulators of the enzyme activity
-
?
additional information
?
-
-
DPP-4 plays a role in the control of immune function, inflammatory responses, and behavior
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
peptide YY + H2O
peptide YY fragment 3-36
-
high affinity substrate of DPP-IV
-
-
?
additional information
?
-
-
obligatory role of the enzyme in renal handling of proline- and hydroxyproline-containing peptides
-
-
?
additional information
?
-
-
binding of dipeptidyl peptidase IV to fibronectin may play a role in interaction of hepatocytes with extracellular matrix in vivo and possibly in matrix assembly
-
-
?
additional information
?
-
-
enzyme is important for metabolic regulation
-
?
additional information
?
-
-
hemorphins may represent endogenous regulators of the enzyme activity
-
?
additional information
?
-
-
DPP-4 plays a role in the control of immune function, inflammatory responses, and behavior
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
-
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
-
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
Diprotin A
dipeptidyl peptidase IV in soluble and membrane-bound fractions from the hypothalamus and hippocampus areas is distinguished kinetically as insensitive and sensitive to diprotin A, respectively
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
-
-
(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
-
-
(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
-
-
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
-
the inhibitor has similar potency to sitagliptin and excellent pharmacokinetic properties
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
-
-
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
-
66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
-
i. e. ABT-279, a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
-
-
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
in vivo plasma DPP-IV inhibition in Wistar rats
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
-
84% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 73% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
-
-
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
-
-
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
-
-
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
-
-
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile
-
potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV, 82% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
85% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
75% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 48% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
64% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 7% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
77% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 56% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
63% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 15% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
89% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 59% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 74% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
-
-
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
30% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 20% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
competitive, reversible inhibitor. Pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
pharmacokinetic parameters
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
-
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
-
-
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
-
-
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
-
-
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-[(3R)-3-aminopiperidin-1-yl]-3-(2-chlorobenzyl)-5-methyl-4-oxo-4,5-dihydro-3H-imidazo[4,5-c]quinoline-8-carboxylate
-
compound shows significantly high oral absorption and potent dipeptidyl peptidase IV inhibition in vivo and decreased Zucker fatty rats glucose levels in the oral glucose tolerance test
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
-
vildagliptin, reversible inhibitor, vildagliptin inhibits DPP4 activity by about 50% at a dosage of 0.3 mg/kg body weight
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
pharmacokinetic data
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
-
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine
-
IC50: 190 nmol/L
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide
-
87% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 31% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
15 nM DPP-IV inhibitor with high selectivity over DPP-II, DPP8 and FAP
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide
-
81% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 60% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
i.e. E3024, selective, and competitive
3-N-[(2S,3S)-2-amino-3-methylpentanoyl]-1,3-thiazolidine
-
in genetically susceptible animals, inhibition of DPP IV increases arterial blood pressure via Y1 receptors when elevated blood pressure is reduced with antihypertensive drugs provided that the sympathetic nervous system is functional
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
-
-
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.8 nmol/L
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 41.3 nmol/L
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 10.8 nmol/L
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 34.5 nmol/L
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 13.0 nmol/L
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 14.8 nmol/L
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 125 nmol/L
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 55.1 nmol/L
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 33.6 nmol/L
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 43.8 nmol/L
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.0 nmol/L
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 30.4 nmol/L
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 54.9 nmol/L
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
-
-
3H-imidazo[4,5-c]quinolin-4(5H)-one
-
inhibitor with potent dipeptidyl peptidase IV inhibitory activity that shows poor oral absorption can be improved by esterification of the carboxylic acid moiety
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
-
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
-
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
-
instability in human and dog plasma, but not in rat plasma. Unstable in fresh rat, dog, and human blood
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
-
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
in vivo plasma DPP-IV inhibition in Wistar rats
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile
-
IC50: 0.27 nmol/L
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile
-
IC50: 2.3 nmol/L
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile
-
IC50: 500 nmol/L
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
-
-
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
inhibition of plasma DPP-4 activity after oral administration
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate
-
AB-192, irreversible inhibitor, AB-192 sufficiently inhibits DPP4 only in the higher dosage range of more than 1mg/kg body weight
Ca2+
-
mixed type inhibition, Ca2+ ions preferentially bind to the betA-propeller domain
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
-
-
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
-
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
-
-
hemorphin-4 peptide
-
12% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWT, competitive
hemorphin-5 peptide
-
18% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQ, competitive
-
hemorphin-7 peptide
-
30% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQRF, selective and competitive
L-Ile-L-Pro-L-Ile
-
the dipeptidyl peptidase IV inhibitor switches the enzyme from hydrolase to synthase functional mode to generate endomorphin 2
LVV-hemorphin-7 peptide
-
9% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence LVVYPWTQRF, the additional leucine residue reduces the inhibitory potential
Lys[Z(NO2)]-pyrrolidide
-
inhibition of DPPIV catalytic activity is associated with inhibition of NHE3-mediated NaHCO3 reabsorption in the native renal proximal tubule
methionyl-2(S)-cyanopyrrolidine
-
irreversible noncompetitive inhibitor of DP-IV
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
-
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide
-
66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
-
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
N3-[2-[(2S)-2-cyanopyrrolidin-1-yl]-1,1-dimethyl-2-oxoethyl]-N-(2-pyridin-2-ylethyl)-b-alaninamide
-
in vivo efficacy in rat models after oral administration
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
-
-
VV-hemorphin-5 peptide
-
10% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQ
VV-hemorphin-6 peptide
-
15% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQR
VV-hemorphin-7 peptide
-
27% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQRF
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
-
-
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
-
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
in vivo efficacy in rat models after oral administration. The inhibitor has potential for further development as antidiabetic agent
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 18% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
88% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 41% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
alogliptin
-
potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, complete inhibition of DPP-4 24 h after treatment with 10 mg/kg alogliptin
BI 1356
-
competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro
BI 1356
-
proposed trade name ONDERO, exhibits a prominent concentration-dependent plasma protein binding due to a saturable high affinity binding to the DPP-4 target in plasma
BI 1356
-
proposed trade name ONDERO, highly potent and selective DPP-4 inhibitor
isoleucine thiazolidide
-
i.e. P32/98. Enhancement of incretin with the DPP-4 inhibitor P32/98 has therapeutic effects in hyperinsulinaemia, hyperglycaemia and impaired glucose toleranceIGT in Zucker rats with incipient impaired glucose tolerance and manifest impaired glucose tolerance. Apparently, administration of P32/98 in Zucker rats with incipient impaired glucose tolerance results in more efficient beta-cell function, which is associated with less need for insulin to cope with deterioration of glucose tolerance. P32/98 has a strong effect on dyslipidaemia in manifest impaired glucose tolerance. P32/98 has no side effect on intestinal growth. Daily intake of P32/98 is a promising strategy for treatment of glucose intolerance and has the potential to prevent type 2 diabetes
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
potent inhibitor of DPP IV
sitagliptin
-
the systemic clearance of sitagliptin in rats is driven primarily by renal elimination of intact parent drug, with contribution from biliary excretion and metabolism (minor). Active transport mechanisms are probably involved in the renal elimination of sitagliptin
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
vildagliptin
-
liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
additional information
conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity
-
additional information
-
inhibitory mechanism, the N-terminus sequence of hemorphins influence the interaction between hemorphins and the enzyme
-
additional information
-
4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles show a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates is found to contribute to their long duration of action
-
additional information
-
in male Zucker diabetic rats, DPP-4 inhibition shows a delay in onset of diabetes and improved glucose tolerance and insulin secretion
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
-
enzyme activity is increased to 166% in starved rats compared to feed rats
-
additional information
-
CCL11 application leads to an up-regulation of DPPIV, which is not associated with negative feedback inhibition via DPPIV-cleaved CCL11(3-74)
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
processing kinetics of wild-type and mutants
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000012
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
0.000001
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
0.000056
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
0.000003
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
0.000001
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000017 - 0.000024
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000002 - 0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000003 - 0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.00000021
(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.000012
(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.000013
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
Rattus norvegicus
-
-
0.000023
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000082
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00013
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.000027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00019
(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00022
(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00015
(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00028
(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00026
(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00023
(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00013
(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.000084
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000145
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000098
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00158
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000128
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000059
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000135
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000076
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000264
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000272
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000021
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000037
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00057
(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.001018
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00000031
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000057
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000004
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000032
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000438
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000123
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000132
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000015
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000805
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000151
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000018
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000087
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00486
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000366
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000511
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.00005
(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00037
(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000058
(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000084
(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00011
(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00038
(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00049
(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00063
(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00078
(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00057
(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00034
(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00061
(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000014
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000023
(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000042
(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000091
(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000046
(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00000018
(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00000043
(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000066
(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000005
(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000043
(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.0000063
(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000131
(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000116
(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00032
(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000113
(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000088
(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000587
(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000045
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000029
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000092
(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000175
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000093
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.000017
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000015
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000298
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000031
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000031
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000013
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000002
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000016
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000025
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000019
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000009
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000014
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000022
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00004
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000035
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000021
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.0016
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
Rattus norvegicus
-
-
0.00149
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
Rattus norvegicus
-
-
0.00009
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
Rattus norvegicus
-
-
0.001165
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000057
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000645
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.00005
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.0000032
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.0000075
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000525
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000203
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000017
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.00004
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.00007
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
Rattus norvegicus
-
-
0.000122
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000019
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.000142
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Rattus norvegicus
-
-
0.000121
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
Rattus norvegicus
-
-
0.00013
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone
Rattus norvegicus
-
IC50: 130 nM
0.0000036
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
Rattus norvegicus
-
-
0.0000551
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.0000549
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000021
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000171
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.00019
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.0000022
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
Rattus norvegicus
-
-
0.000638
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00071
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002228
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000698
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001459
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.004767
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.003755
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001022
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001449
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.006677
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002701
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001631
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00176
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.012
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000037
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
Rattus norvegicus
-
-
0.000011
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
Rattus norvegicus
-
-
0.00000032
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00043
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
-
0.0000072
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000072
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000103
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000109
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000175
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000762
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.0000014
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000169
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000176
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000029
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
Rattus norvegicus
-
-
0.000009
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000031
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000011
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000314
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000383
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000811
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000151
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.0000176
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000035
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000039
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000019
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
Rattus norvegicus
-
-
0.0000037
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
Rattus norvegicus
-
-
0.00043
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
Rattus norvegicus
-
-
0.000022 - 0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
0.0000998
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
Rattus norvegicus
-
-
0.0000047
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
Rattus norvegicus
-
-
0.0000018
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
Rattus norvegicus
-
-
0.0000744
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000019
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000008
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000015
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000029
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.00003
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000018
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000195 - 0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000165
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
Rattus norvegicus
-
-
0.0000028
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000377
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
-
0.00051
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
Rattus norvegicus
-
-
0.001027
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
Rattus norvegicus
-
-
0.000185
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
Rattus norvegicus
-
-
0.00009 - 0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
0.000143
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
Rattus norvegicus
-
-
0.000523
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
Rattus norvegicus
-
-
0.000506
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
Rattus norvegicus
-
-
0.000217 - 0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
0.000415
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
Rattus norvegicus
-
-
0.000468
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
Rattus norvegicus
-
-
0.000308
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
Rattus norvegicus
-
-
0.000817
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.0000012
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.000026
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000056
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000047
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00006
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000084
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000068
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000063
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000101
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000075
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000042
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000064
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000073
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000086
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000054
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000016
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000027
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000015
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000017
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000021
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000026
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00002
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000022
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000019
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000024
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000142
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
Rattus norvegicus
-
-
0.0000093
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
Rattus norvegicus
-
-
0.0000033
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.0000125
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000136
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000343
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.000168
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.0000341
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.0000096
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.0000189
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
Rattus norvegicus
-
-
0.0000018
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
Rattus norvegicus
-
-
0.0000336
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
Rattus norvegicus
-
-
0.0000107
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000134
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000101
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000061
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000103
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000019
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.00078
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
Rattus norvegicus
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
0.000234
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
Rattus norvegicus
-
-
0.00000236
ASP-8497
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.000031
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
Rattus norvegicus
-
-
0.000219
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.00019
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.0000153
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
Rattus norvegicus
-
-
0.00115
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
Rattus norvegicus
-
-
0.000134
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000119 - 0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.000359
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000258
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000023
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
Rattus norvegicus
-
-
0.0002
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000226
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00049
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.03845
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000088 - 0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.00011 - 0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000049
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
Rattus norvegicus
-
-
0.000077
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
Rattus norvegicus
-
-
0.00009
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000047
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
Rattus norvegicus
-
-
0.000087
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
Rattus norvegicus
-
-
0.000066
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
Rattus norvegicus
-
-
0.000009
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.000014
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.00000038
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000012
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.00003
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.000024
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000053
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000094
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.00002
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000034
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.01
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
Rattus norvegicus
-
-
0.0000026 - 0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
Rattus norvegicus
-
-
0.00051
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
Rattus norvegicus
-
-
0.0022
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
Rattus norvegicus
-
-
0.00133
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
Rattus norvegicus
-
-
0.000236
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.00000171
saxagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.001534
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.004149
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001793
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001228
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00083
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00079
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000667
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000866
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.0000163
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
Rattus norvegicus
-
-
0.000069
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
Rattus norvegicus
-
-
0.000017
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000024
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000002
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000003
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000022
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0000195
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.00009
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000217
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.000119
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000088
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00011
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.0000026
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.0000093
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.0000115
sitagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00003
sitagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00000167
vildagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.000051
vildagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6.5 - 9.5
-
pH 6.5: about 60% of maximal activity, pH 9.5: about 45% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
-
664313, 664847, 678597, 678634, 678658, 681319, 681325, 696134, 696136, 696668, 696746, 697764, 699445, 699748, 702514, 702623, 704840
-
mRNA expression in ipsilateral and contralateral cortices. At day 3 post-ischemia, dipeptidyl peptidase IV, 8 and aminopeptidase N are identified in activated microglia and macrophages in the ipsilateral cortex. Seven days post artery occlusion, dipeptidyl peptidase IV immunoreactivity is found in the perikarya of surviving cortical neurons of the ipsilateral hemisphere. At the same time point, dipeptidyl peptidase IV, 8 and aminopeptidase N are targeted in astroglial cells. Total dipeptidyl peptidase IV, 8 and 9 activities remain constant in both hemispheres until day 3 post experimental ischemia, but are increased to 165% in the ipsilateral cortex at day 7
-
maximally expressed in mid-villus cells, substantial activity in the crypt cells, primarily associated with brush border membranes in all segments, in the proximal intestine, a significant amount of the enzyme is associated with the cytosol fraction. Cytosol and brush border membrane forms are immunologically identical
additional information
-
DPPIV expression is greatly decreased or lost in cells derived from neuroblastoma
-
dipeptidyl peptidase IV is expressed in the renal microcirculation. Inhibition of this ecto-enzyme causes arterial peptide YY1-36 to more effectively enhance angiotensin II-induced renal vasoconstriction in genetically susceptible kidneys
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
membrane-bound form, 60%, and a soluble form, 40%. The main protein portion of the enzyme having the antigenic sites is located on the inside surface of lysosomes
-
renal brush-border membrane of Fisher 344 rats from the Japanese Charles River Inc. specifically lacks dipeptidyl peptidase IV (DPP IV) activity whereas the renal brush border membrane of Fischer 344 rats from three different sources within the United States possesses normal levels of activity
-
localized in the apical domain of the plasma membrane
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
physiological function
DPP-IV is released from muscle and induces an order-dependent increase in arteriolar diameter, with the largest change in the 6A arterioles. DPP-IV appears to act on neuropeptide Y to attenuate vasoconstriction
malfunction
-
DPP4-deficient rats are resistant to developing diabetes, while susceptible to dyslipidaemia and reduction of glomerular filtration rate by streptozotocin
physiological function
physiological function
-
DPP4 activation may be responsible for hyperglycaemia, lipid metabolism and preservation of renal function
physiological function
-
DPPIV promotes apoptosis in neuroblastoma cells through caspase activation and decreased Akt phosphorylation, and inhibits stromal-derived factor 1-mediated in vitro cell migration and angiogenic potential. DPPIV plays a potential role in inhibiting neuroblastoma growth and progression
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). DPP4_RAT
767
1
88089
Swiss-Prot
Secretory Pathway (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
105000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
additional information
domain structure involving cysteine residues and disulfide bridges, structure-function relationship, overview, cysteine residues 326, 337,445, 448, 455, 473, and 552 are essential for the correct folding and intracellular trafficking of the enzyme, structure of wild-type compared to the mutant enzymes
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phosphoprotein
DPP IV is tyrosine-phosphorylated in an insulin-dependent manner in hepatic endosomal fractions. Possible involvement of luminal cellular tyrosine kinase in this process
no modification
-
the signal peptide of dipeptidyl peptidase IV is not cleaved off during biosynthesis but functions as the membrane-anchoring domain even in the mature form
side-chain modification
additional information
-
two-fold activation of precursor enzyme form occurs during transfer from the Golgi membranes to the brush border membranes
side-chain modification
-
glycoprotein
side-chain modification
-
carbohydrate structure of the high-mannose type and of the complex type. No detectable O-linked glycosylation on the enzyme in the transfected cells
side-chain modification
-
contains 5.4 sugar chains per mol of enzyme. A mixture of 26 monoantennary, biantennary, triantennary and tetraantennary complex type sugar chains. The complex-type sugar chains all contain the bisecting N-acetylglucosamine residue and are incompletely galactosylated in their outer-chain moieties
side-chain modification
-
the glycoprotein is characterized by an intramolecular heterogenous turnover of the protein backbone and carbohydrate chain. The faster turnover of the carbohydrate chain is restricted only to the outer sugar. The inner core sugar D-mannose and N-acetyl-D-glucosamine turn over at the same rate as the protein backbone
side-chain modification
-
sialoglycoprotein, sialyl residues represent termini of N-linked complex-type oligosaccharides
side-chain modification
-
contains 12.4% carbohydrate. The carbohydrate moiety is composed of mannose, galactose, fucose, N-acetylglucosamine and neuraminic acid in a molar ratio 14:17:2:24:11. The enzyme does not contain O-linked oligosaccharide chains
side-chain modification
-
contains 8% carbohydrate per weight. Fucose, galactose, glucose, mannose, sialic acid and hexosamine sugars are present. The asparagine linked oligosaccharide side chains contain approximately 19 sugar residues
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
C326G
site-directed mutagenesis, total inhibition of surface expression, catalytically inactive, half-life of the mutant enzyme is reduced by over 90%
C337S
site-directed mutagenesis, weak expression, reduced activity, half-life of the mutant enzyme is reduced by over 90%
C445S
site-directed mutagenesis, total inhibition of surface expression, catalytically inactive, half-life of the mutant enzyme is reduced by over 90%
C448S
site-directed mutagenesis, total inhibition of surface expression, catalytically inactive, half-life of the mutant enzyme is reduced by over 90%
C455G
site-directed mutagenesis, weak expression, reduced activity, half-life of the mutant enzyme is reduced by over 90%
C473S
site-directed mutagenesis, weak expression, reduced activity, half-life of the mutant enzyme is reduced by over 90%
C552S
site-directed mutagenesis, weak expression, reduced activity, half-life of the mutant enzyme is reduced by over 90%
additional information
-
mutant strain harboring a mutation which leads to rapid degradation of the enzyme
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
45
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
monosodium glutamate and/or food deprivation decreases the activity of DPPIV insensitive to diprotin A in the soluble and membrane-bound fraction from the hypothalamus, as well as the activity of DPPIV sensitive to diprotin A in the soluble fraction from the hypothalamus and in the membrane-bound fraction from the hippocampus
monosodium glutamate and/or food deprivation increases the activity of DPPIV insensitive to diprotin A in the membrane-bound fraction from the hippocampus
both high-fat and high-sucrose diet-fed rats show significantly higher plasma DPP IV activity than normal diet-fed rats in the order of high-fat diet>high-sucrose diet>normal diet
-
high-fat and high-sucrose diets do not significantly affect DPP IV activity and mRNA expression in the kidney
-
high-fat, but not high-sucrose diet causes a significant decrease in DPP IV activity in the liver as compared to the control
-
plasma DPP4 activity increases progressively with time after streptozotocin treatment in wild type rats, the kidney of wild type rats show decreased DPP4 activity with increased Dpp4 mRNA after streptozotocin treatment
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
veterinary medicine
medicine
-
specific inhibition of the enzyme shows efficacy in the treatment of type 2 diabetes
medicine
-
inhibition of DPP-IV can be an effective approach to treat type 2 diabetes mellitus by potentiating insulin secretion. 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, i.e. KR-62436, could be good lead compound for further development as a new anti-diabetic agent
medicine
-
a DPP-IV inhibitor (3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate) in combination with glybenclamide or nateglinide may be a promising option for the treatment of type 2 diabetes, and particularly, for controlling postprandial hyperglycemia in the clinic
medicine
-
genetic or environmental factors that decrease DPPIV activity might increase the risk of angiotensin-converting enzyme inhibitor-associated angioedema
medicine
-
imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabete, pharmacokinetic properties
medicine
-
in genetically susceptible animals, inhibition of DPP IV increases arterial blood pressure via Y1 receptors when elevated blood pressure is reduced with antihypertensive drugs provided that the sympathetic nervous system is functional
medicine
-
mRNA expression in ipsilateral and contralateral cortices. At day 3 post-ischemia, dipeptidyl peptidase IV, 8 and aminopeptidase N are identified in activated microglia and macrophages in the ipsilateral cortex. Seven days post artery occlusion, dipeptidyl peptidase IV immunoreactivity is found in the perikarya of surviving cortical neurons of the ipsilateral hemisphere. At the same time point, dipeptidyl peptidase IV, 8 and aminopeptidase N are targeted in astroglial cells. Total dipeptidyl peptidase IV, 8 and 9 activities remain constant in both hemispheres until day 3 post experimental ischemia, but are increased to 165% in the ipsilateral cortex at day 7. Dipeptidyl peptidase II and aminopeptidase N are up-regulated ipsilaterally from 6 h to 7 days post ischemia. IPC1755, a non-selective protease inhibitor, reveals a significant reduction of cortical lesions after transient cerebral ischemia
veterinary medicine
-
inhibition of intragraft DPP IV enzymatic activity significantly reduces ischemia/reperfusion-associated pulmonary injury, allowing for successful transplantation after 18 h of ischemia
veterinary medicine
-
inhibiting intragraft DPP IV enzymatic activity in a rat single-lung transplantation model abolishes ischemia/reperfusion injury after extended ischemia
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Tiruppathi, C.; Miyamoto, Y.; Ganapathy, V.; Roesel, R.A.; Whitford, G.M.; Leibach, F.H.
Hydrolysis and transport of proline-containing peptides in renal brush-border membrane vesicles from dipeptidyl peptidase IV-positive and dipeptidyl peptidase IV-negative rat strains
J. Biol. Chem.
265
1476-1483
1990
Rattus norvegicus
Ogata, S.; Misumi, Y.; Ikehara, Y.
Primary structure of rat liver dipeptidyl peptidase IV deduced from its cDNA and identification of the NH2-terminal signal sequence as the membrane-anchoring domain
J. Biol. Chem.
264
3596-3601
1989
Rattus norvegicus
Reuter, W.; Hartel, S.; Hanski, C.; Huhle, T.; Zimmer, T.; Gossrau, R.
Biochemical properties of dipeptidyl peptidase IV in liver and hepatoma plasma membranes
Adv. Enzyme Regul.
28
253-269
1989
Rattus norvegicus
Hong, W.; Piazza, G.A.; Hixson, D.C.; Doyle, D.
Expression of enzymatically active rat dipeptidyl peptidase IV in Chinese hamster ovary cells after transfection
Biochemistry
28
8474-8479
1989
Rattus norvegicus
Piazza, G.A.; Callanan, H.M.; Mowery, J.; Hixson, D.C.
Evidence for a role of dipeptidyl peptidase IV in fibronectin-mediated interactions of hepatocytes with extracellular matrix
Biochem. J.
262
327-334
1989
Rattus norvegicus
Kikuchi, M.; Fukuyama, K.; Epstein, W.L.
Soluble dipeptidyl peptidase IV from terminal differentiated rat epidermal cells: purification and its activity on synthetic and natural peptides
Arch. Biochem. Biophys.
266
369-376
1988
Rattus norvegicus
Yamashita, K.; Tachibana, Y.; Matsuda, Y.; Katunuma, N.; Kochibe, N.; Kobata, A.
Comparative studies of the sugar chains of aminopeptidase N and dipeptidylpeptidase IV purified from rat kidney brush-border membrane
Biochemistry
27
5565-5573
1988
Rattus norvegicus
Hartel, S.; Hanski, C.; Kreisel, W.; Hoffmann, C.; Mauck, J.; Reutter, W.
Rapid purification of dipeptidyl peptidase IV from rat liver plasma membrane
Biochim. Biophys. Acta
924
543-547
1987
Rattus norvegicus
Hanski, C.; Zimmer, T.; Gossrau, R.; Reutter, W.
Increased activity of dipeptidyl peptidase IV in serum of hepatoma-bearing rats coincides with the loss of the enzyme from the hepatoma plasma membrane
Experientia
42
826-828
1986
Rattus norvegicus
Bartles, J.R.; Braiterman, L.T.; Hubbard, A.L.
Biochemical characterization of domain-specific glycoproteins of the rat hepatocyte plasma membrane
J. Biol. Chem.
260
12792-12802
1985
Rattus norvegicus
Umezawa, H.; Aoyagi, T.; Ogawa, K.; Naganawa, H.; Hamada, M.; Takeuchi, T.
Diprotins A and B, inhibitors of dipeptidyl aminopeptidase IV, produced by bacteria
J. Antibiot.
37
422-425
1984
Rattus norvegicus
Heins, J.; Neubert, K.; Barth, A.; Canizaro, P.C.; Behal, F.J.
Kinetic investigation of the hydrolysis of aminoacyl p-nitroanilides by dipeptidyl peptidase IV from human and pig kidney
Biochim. Biophys. Acta
785
30-35
1984
Homo sapiens, Rattus norvegicus, Sus scrofa
Miura, S.; Song, I.S.; Morita, A.; Erickson, R.H.; Kim, Y.S.
Distribution and biosynthesis of aminopeptidase N and dipeptidyl aminopeptidase IV in rat small intestine
Biochim. Biophys. Acta
761
66-75
1983
Rattus norvegicus
Erickson, R.H.; Bella, A.M.; Brophy, E.J.; Kobata, A.; Kim, Y.S.
Purification and molecular characterization of rat intestinal brush border membrane dipeptidyl aminopeptidase IV
Biochim. Biophys. Acta
756
258-265
1983
Rattus norvegicus
Bella, A.M.; Erickson, R.H.; Kim, Y.S.
Rat intestinal brush border membrane dipeptidyl-aminopeptidase IV: kinetic properties and substrate specificities of the purified enzyme
Arch. Biochem. Biophys.
218
156-162
1982
Rattus norvegicus
Kyouden, T.; Himeno, M.; Ishikawa, T.; Ohsumi, Y.; Kato, K.
Purification and characterization of dipeptidyl peptidase IV in rat liver lysosomal membranes
J. Biochem.
111
770-777
1992
Rattus norvegicus
Volk, B.A.; Kreisel, W.; Kttgen, E.; Gerok, W.; Reutter, W.
Heterogeneous turnover of terminal and core sugars within the carbohydrate chain of dipeptidylaminopeptidase IV isolated from rat liver plasma membrane
FEBS Lett.
163
150-152
1983
Rattus norvegicus
Ikehara, Y.; Ogata, S.; Misumi, Y.
Dipeptidyl-peptidase IV from rat liver
Methods Enzymol.
244
215-227
1994
Rattus norvegicus
Cohen, M.; Fruitier-Arnaudin, I.; Piot, J.M.
Hemorphins: substrates and/or inhibitors of dipeptidyl peptidase IV. Hemorphins N-terminus sequence influence on the interaction between hemorphins and DPPIV
Biochimie
86
31-37
2004
Rattus norvegicus
Rosenblum, J.S.; Kozarich, J.W.
Prolyl peptidases: a serine protease subfamily with high potential for drug discovery
Curr. Opin. Chem. Biol.
7
496-504
2003
Homo sapiens, Mammalia, Mus musculus, Rattus norvegicus, Sus scrofa
Dobers, J.; Grams, S.; Reutter, W.; Fan, H.
Roles of cysteines in rat dipeptidyl peptidase IV/CD26 in processing and proteolytic activity
Eur. J. Biochem.
267
5093-5100
2000
no activity in Cricetulus griseus, Rattus norvegicus (P14740)
Ihara, T.; Tsujikawa, T.; Fujiyama, Y.; Ueyama, H.; Bamba, T.; Ohkubo, I.
Enhancement of brush border peptidase activity in rat jejunum during starvation
Int. Congr. Ser.
1218
389-393
2001
Rattus norvegicus
-
Longenecker, K.L.; Stewart, K.D.; Madar, D.J.; Jakob, C.G.; Fry, E.H.; Wilk, S.; Lin, C.W.; Ballaron, S.J.; Stashko, M.A.; Lubben, T.H.; Yong, H.; Pireh, D.; Pei, Z.; Basha, F.; Wiedeman, P.E.; von Geldern, T.W.; Trevillyan, J.M.; Stoll, V.S.
Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors
Biochemistry
45
7474-7482
2006
Homo sapiens, Rattus norvegicus (P14740)
Abe, M.; Akiyama, T.; Umezawa, Y.; Yamamoto, K.; Nagai, M.; Yamazaki, H.; Ichikawa, Y.; Muraoka, Y.
Synthesis and biological activity of sulphostin analogues, novel dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem.
13
785-797
2005
Rattus norvegicus
Sakashita, H.; Akahoshi, F.; Kitajima, H.; Tsutsumiuchi, R.; Hayashi, Y.
[(S)-gamma-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors
Bioorg. Med. Chem.
14
3662-3671
2006
Homo sapiens, Rattus norvegicus
Kim, K.R.; Rhee, S.D.; Kim, H.Y.; Jung, W.H.; Yang, S.D.; Kim, S.S.; Ahn, J.H.; Cheon, H.G.
KR-62436, 6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile, is a novel dipeptidyl peptidase-IV (DPP-IV) inhibitor with anti-hyperglycemic activity
Eur. J. Pharmacol.
518
63-70
2005
Homo sapiens, Rattus norvegicus, Sus scrofa
Bilodeau, N.; Fiset, A.; Poirier, G.G.; Fortier, S.; Gingras, M.C.; Lavoie, J.N.; Faure, R.L.
Insulin-dependent phosphorylation of DPP IV in liver. Evidence for a role of compartmentalized c-Src
FEBS J.
273
992-1003
2006
Rattus norvegicus (P14740)
Girardi, A.C.; Fukuda, L.E.; Rossoni, L.V.; Malnic, G.; Reboucas, N.A.
Dipeptidyl peptidase IV inhibition downregulates Na+ - H+ exchanger NHE3 in rat renal proximal tubule
Am. J. Physiol. Renal Physiol.
294
F414-F422
2008
Rattus norvegicus
Kondo, T.; Nekado, T.; Sugimoto, I.; Ochi, K.; Takai, S.; Kinoshita, A.; Tajima, Y.; Yamamoto, S.; Kawabata, K.; Nakai, H.; Toda, M.
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration
Bioorg. Med. Chem.
15
2631-2650
2007
Homo sapiens, Rattus norvegicus
Kondo, T.; Sugimoto, I.; Nekado, T.; Ochi, K.; Ohtani, T.; Tajima, Y.; Yamamoto, S.; Kawabata, K.; Nakai, H.; Toda, M.
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV
Bioorg. Med. Chem.
15
2715-2735
2007
Homo sapiens, Rattus norvegicus
Sakashita, H.; Akahoshi, F.; Yoshida, T.; Kitajima, H.; Hayashi, Y.; Ishii, S.; Takashina, Y.; Tsutsumiuchi, R.; Ono, S.
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors
Bioorg. Med. Chem.
15
641-655
2007
Rattus norvegicus, Homo sapiens (P27487)
Kondo, T.; Nekado, T.; Sugimoto, I.; Ochi, K.; Takai, S.; Kinoshita, A.; Hatayama, A.; Yamamoto, S.; Kawabata, K.; Nakai, H.; Toda, M.
Discovery of long-acting N-(cyanomethyl)-N-alkyl-L-prolinamide inhibitors of dipeptidyl peptidase IV
Bioorg. Med. Chem.
16
190-208
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Tsai, T.Y.; Coumar, M.S.; Hsu, T.; Hsieh, H.P.; Chien, C.H.; Chen, C.T.; Chang, C.N.; Lo, Y.K.; Wu, S.H.; Huang, C.Y.; Huang, Y.W.; Wang, M.H.; Wu, H.Y.; Lee, H.J.; Chen, X.; Chao, Y.S.; Jiaang, W.T.
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem. Lett.
16
3268-3272
2006
Homo sapiens, Rattus norvegicus, Rattus norvegicus Wistar
Kurukulasuriya, R.; Rohde, J.J.; Szczepankiewicz, B.G.; Basha, F.; Lai, C.; Jae, H.S.; Winn, M.; Stewart, K.D.; Longenecker, K.L.; Lubben, T.W.; Ballaron, S.J.; Sham, H.L.; von Geldern, T.W.
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem. Lett.
16
6226-6230
2006
Homo sapiens, Rattus norvegicus (P14740)
Coumar, M.S.; Chang, C.N.; Chen, C.T.; Chen, X.; Chien, C.H.; Tsai, T.Y.; Cheng, J.H.; Wu, H.Y.; Han, C.H.; Wu, S.H.; Huang, Y.W.; Hsu, T.; Hsu, L.J.; Chao, Y.S.; Hsieh, H.P.; Jiaang, W.T.
3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes
Bioorg. Med. Chem. Lett.
17
1274-1279
2007
Rattus norvegicus
Backes, B.J.; Longenecker, K.; Hamilton, G.L.; Stewart, K.; Lai, C.; Kopecka, H.; von Geldern, T.W.; Madar, D.J.; Pei, Z.; Lubben, T.H.; Zinker, B.A.; Tian, Z.; Ballaron, S.J.; Stashko, M.A.; Mika, A.K.; Beno, D.W.; Kempf-Grote, A.J.; Black-Schaefer, C.; Sham, H.L.; Trevillyan, J.M.
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit
Bioorg. Med. Chem. Lett.
17
2005-2012
2007
Rattus norvegicus (P14740), Homo sapiens (P27487)
Yoshida, T.; Sakashita, H.; Akahoshi, F.; Hayashi, Y.
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors
Bioorg. Med. Chem. Lett.
17
2618-2621
2007
Homo sapiens, Rattus norvegicus
Kim, D.; Kowalchick, J.E.; Edmondson, S.D.; Mastracchio, A.; Xu, J.; Eiermann, G.J.; Leiting, B.; Wu, J.K.; Pryor, K.D.; Patel, R.A.; He, H.; Lyons, K.A.; Thornberry, N.A.; Weber, A.E.
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate)
Bioorg. Med. Chem. Lett.
17
3373-3377
2007
Rattus norvegicus
Biftu, T.; Scapin, G.; Singh, S.; Feng, D.; Becker, J.W.; Eiermann, G.; He, H.; Lyons, K.; Patel, S.; Petrov, A.; Sinha-Roy, R.; Zhang, B.; Wu, J.; Zhang, X.; Doss, G.A.; Thornberry, N.A.; Weber, A.E.
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin
Bioorg. Med. Chem. Lett.
17
3384-3387
2007
Canis lupus familiaris, Macaca mulatta, Rattus norvegicus
Koo, K.D.; Kim, M.J.; Kim, S.; Kim, K.H.; Hong, S.Y.; Hur, G.C.; Yim, H.J.; Kim, G.T.; Han, H.O.; Kwon, O.H.; Kwon, T.S.; Koh, J.S.; Lee, C.S.
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones
Bioorg. Med. Chem. Lett.
17
4167-4172
2007
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Biftu, T.; Feng, D.; Qian, X.; Liang, G.B.; Kieczykowski, G.; Eiermann, G.; He, H.; Leiting, B.; Lyons, K.; Petrov, A.; Sinha-Roy, R.; Zhang, B.; Scapin, G.; Patel, S.; Gao, Y.D.; Singh, S.; Wu, J.; Zhang, X.; Thornberry, N.A.; Weber, A.E.
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Bioorg. Med. Chem. Lett.
17
49-52
2007
Canis lupus familiaris, Mus musculus, Rattus norvegicus
Chen, P.; Caldwell, C.G.; Mathvink, R.J.; Leiting, B.; Marsilio, F.; Patel, R.A.; Wu, J.K.; He, H.; Lyons, K.A.; Thornberry, N.A.; Weber, A.E.
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes
Bioorg. Med. Chem. Lett.
17
5853-5857
2007
Rattus norvegicus
Corbett, J.W.; Dirico, K.; Song, W.; Boscoe, B.P.; Doran, S.D.; Boyer, D.; Qiu, X.; Ammirati, M.; Vanvolkenburg, M.A.; McPherson, R.K.; Parker, J.C.; Cox, E.D.
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
Bioorg. Med. Chem. Lett.
17
6707-6713
2007
Rattus norvegicus, Homo sapiens (P27487), Homo sapiens
Edmondson, S.D.; Wei, L.; Xu, J.; Shang, J.; Xu, S.; Pang, J.; Chaudhary, A.; Dean, D.C.; He, H.; Leiting, B.; Lyons, K.A.; Patel, R.A.; Patel, S.B.; Scapin, G.; Wu, J.K.; Beconi, M.G.; Thornberry, N.A.; Weber, A.E.
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem. Lett.
18
2409-2413
2008
Rattus norvegicus
Jackson, E.K.; Dubinion, J.H.; Mi, Z.
Effects of dipeptidyl peptidase iv inhibition on arterial blood pressure
Clin. Exp. Pharmacol. Physiol.
35
29-34
2008
Rattus norvegicus
Raun, K.; von Voss, P.; Gotfredsen, C.F.; Golozoubova, V.; Rolin, B.; Knudsen, L.B.
Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not
Diabetes
56
8-15
2007
Rattus norvegicus
Drucker, D.J.
Dipeptidyl peptidase-4 inhibition and the treatment of type 2 diabetes: preclinical biology and mechanisms of action
Diabetes Care
30
1335-1343
2007
Homo sapiens, Mus musculus, Rattus norvegicus, Sus scrofa
McKennon, S.A.; Campbell, R.K.
The physiology of incretin hormones and the basis for DPP-4 inhibitors
Diabetes Educ.
33
55-66
2007
Homo sapiens, Rattus norvegicus
Augstein, P.; Berg, S.; Heinke, P.; Altmann, S.; Salzsieder, E.; Demuth, H.U.; Freyse, E.J.
Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance
Diabetes Obes. Metab.
10
850-861
2008
Rattus norvegicus
Beconi, M.G.; Reed, J.R.; Teffera, Y.; Xia, Y.Q.; Kochansky, C.J.; Liu, D.Q.; Xu, S.; Elmore, C.S.; Ciccotto, S.; Hora, D.F.; Stearns, R.A.; Vincent, S.H.
Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs
Drug Metab. Dispos.
35
525-532
2007
Canis lupus familiaris, Homo sapiens, Rattus norvegicus
Green, B.D.; Flatt, P.R.; Bailey, C.J.
Inhibition of dipeptidylpeptidase IV activity as a therapy of type 2 diabetes
Expert. Opin. Emerg. Drugs
11
525-539
2006
Homo sapiens, Mus musculus, Rattus norvegicus
Byrd, J.B.; Shreevatsa, A.; Putlur, P.; Foretia, D.; McAlexander, L.; Sinha, T.; Does, M.D.; Brown, N.J.
Dipeptidyl peptidase IV deficiency increases susceptibility to angiotensin-converting enzyme inhibitor-induced peritracheal edema
J. Allergy Clin. Immunol.
120
403-408
2007
Rattus norvegicus
Zhai, W.; Cardell, M.; De Meester, I.; Augustyns, K.; Hillinger, S.; Inci, I.; Arni, S.; Jungraithmayr, W.; Scharpe, S.; Weder, W.; Korom, S.
Intragraft DPP IV inhibition attenuates post-transplant pulmonary ischemia/reperfusion injury after extended ischemia
J. Heart Lung Transplant.
26
174-180
2007
Rattus norvegicus
Madar, D.J.; Kopecka, H.; Pireh, D.; Yong, H.; Pei, Z.; Li, X.; Wiedeman, P.E.; Djuric, S.W.; Von Geldern, T.W.; Fickes, M.G.; Bhagavatula, L.; McDermott, T.; Wittenberger, S.; Richards, S.J.; Longenecker, K.L.; Stewart, K.D.; Lubben, T.H.; Ballaron, S.J.; Stashko, M.A.; Long, M.A.; Wells, H.; Zinker, B.A.
Discovery of (2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes
J. Med. Chem.
49
6416-6420
2006
Canis lupus familiaris, Rattus norvegicus, Homo sapiens (P27487)
Feng, J.; Zhang, Z.; Wallace, M.B.; Stafford, J.A.; Kaldor, S.W.; Kassel, D.B.; Navre, M.; Shi, L.; Skene, R.J.; Asakawa, T.; Takeuchi, K.; Xu, R.; Webb, D.R.; Gwaltney, S.L.
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
J. Med. Chem.
50
2297-2300
2007
Rattus norvegicus
Eckhardt, M.; Langkopf, E.; Mark, M.; Tadayyon, M.; Thomas, L.; Nar, H.; Pfrengle, W.; Guth, B.; Lotz, R.; Sieger, P.; Fuchs, H.; Himmelsbach, F.
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
J. Med. Chem.
50
6450-6453
2007
Canis lupus familiaris, Macaca mulatta, Rattus norvegicus, Homo sapiens (P27487)
Kim, D.; Kowalchick, J.E.; Brockunier, L.L.; Parmee, E.R.; Eiermann, G.J.; Fisher, M.H.; He, H.; Leiting, B.; Lyons, K.; Scapin, G.; Patel, S.B.; Petrov, A.; Pryor, K.D.; Roy, R.S.; Wu, J.K.; Zhang, X.; Wyvratt, M.J.; Zhang, B.B.; Zhu, L.; Thornberry, N.A.; Weber, A.E.
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines
J. Med. Chem.
51
589-602
2008
Rattus norvegicus
Yamazaki, K.; Yasuda, N.; Inoue, T.; Yamamoto, E.; Sugaya, Y.; Nagakura, T.; Shinoda, M.; Clark, R.; Saeki, T.; Tanaka, I.
Effects of the combination of a dipeptidyl peptidase IV inhibitor and an insulin secretagogue on glucose and insulin levels in mice and rats
J. Pharmacol. Exp. Ther.
320
738-746
2007
Mus musculus, Rattus norvegicus
Jackson, E.K.; Zhang, M.; Liu, W.; Mi, Z.
Inhibition of renal dipeptidyl peptidase IV enhances peptide YY1-36-induced potentiation of angiotensin II-mediated renal vasoconstriction in spontaneously hypertensive rats
J. Pharmacol. Exp. Ther.
323
431-437
2007
Rattus norvegicus
Zhai, W.; Cardell, M.; De Meester, I.; Augustyns, K.; Hillinger, S.; Inci, I.; Arni, S.; Jungraithmayr, W.; Scharpe, S.; Weder, W.; Korom, S.
Ischemia/reperfusion injury: The role of CD26/dipeptidyl-peptidase-IV-inhibition in lung transplantation
Transplant. Proc.
38
3369-3371
2006
Rattus norvegicus
Matsuyama-Yokono, A.; Tahara, A.; Nakano, R.; Someya, Y.; Nagase, I.; Hayakawa, M.; Shibasaki, M.
ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity
Biochem. Pharmacol.
76
98-107
2008
Canis lupus familiaris, Homo sapiens, Mus musculus, Rattus norvegicus
Jost, M.M.; Lamerz, J.; Tammen, H.; Menzel, C.; De Meester, I.; Lambeir, A.M.; Augustyns, K.; Scharpe, S.; Zucht, H.D.; Rose, H.; Juergens, M.; Schulz-Knappe, P.; Budde, P.
In vivo profiling of DPP4 inhibitors reveals alterations in collagen metabolism and accumulation of an amyloid peptide in rat plasma
Biochem. Pharmacol.
77
228-237
2009
Homo sapiens, Rattus norvegicus
Eckhardt, M.; Hauel, N.; Himmelsbach, F.; Langkopf, E.; Nar, H.; Mark, M.; Tadayyon, M.; Thomas, L.; Guth, B.; Lotz, R.
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors
Bioorg. Med. Chem. Lett.
18
3158-3162
2008
Homo sapiens, Rattus norvegicus
Tsai, T.Y.; Hsu, T.; Chen, C.T.; Cheng, J.H.; Chiou, M.C.; Huang, C.H.; Tseng, Y.J.; Yeh, T.K.; Huang, C.Y.; Yeh, K.C.; Huang, Y.W.; Wu, S.H.; Wang, M.H.; Chen, X.; Chao, Y.S.; Jiaang, W.T.
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem. Lett.
19
1908-1912
2009
Rattus norvegicus
Tsai, T.Y.; Hsu, T.; Chen, C.T.; Cheng, J.H.; Yeh, T.K.; Chen, X.; Huang, C.Y.; Chang, C.N.; Yeh, K.C.; Hsieh, S.H.; Chien, C.H.; Chang, Y.W.; Huang, C.H.; Huang, Y.W.; Huang, C.L.; Wu, S.H.; Wang, M.H.; Lu, C.T.; Chao, Y.S.; Jiaang, W.T.
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
Bioorg. Med. Chem.
17
2388-2399
2009
Rattus norvegicus
Lee, B.; Shi, L.; Kassel, D.B.; Asakawa, T.; Takeuchi, K.; Christopher, R.J.
Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys
Eur. J. Pharmacol.
589
306-314
2008
Canis lupus familiaris, Macaca fascicularis, Homo sapiens, Rattus norvegicus
Forssmann, U.; Stoetzer, C.; Stephan, M.; Kruschinski, C.; Skripuletz, T.; Schade, J.; Schmiedl, A.; Pabst, R.; Wagner, L.; Hoffmann, T.; Kehlen, A.; Escher, S.E.; Forssmann, W.G.; Elsner, J.; von Hoersten, S.
Inhibition of CD26/dipeptidyl peptidase IV enhances CCL11/eotaxin-mediated recruitment of eosinophils in vivo
J. Immunol.
181
1120-1127
2008
Homo sapiens, Rattus norvegicus
Connolly, B.A.; Sanford, D.G.; Chiluwal, A.K.; Healey, S.E.; Peters, D.E.; Dimare, M.T.; Wu, W.; Liu, Y.; Maw, H.; Zhou, Y.; Li, Y.; Jin, Z.; Sudmeier, J.L.; Lai, J.H.; Bachovchin, W.W.
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety
J. Med. Chem.
51
6005-6013
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Fuchs, H.; Tillement, J.P.; Urien, S.; Greischel, A.; Roth, W.
Concentration-dependent plasma protein binding of the novel dipeptidyl peptidase 4 inhibitor BI 1356 due to saturable binding to its target in plasma of mice, rats and humans
J. Pharm. Pharmacol.
61
55-62
2009
Homo sapiens, Mus musculus, Rattus norvegicus
Thomas, L.; Eckhardt, M.; Langkopf, E.; Tadayyon, M.; Himmelsbach, F.; Mark, M.
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with oth
J. Pharmacol. Exp. Ther.
325
175-182
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Michel, M.C.; Fliers, E.; Van Noorden, C.J.
Dipeptidyl peptidase IV inhibitors in diabetes: more than inhibition of glucagon-like peptide-1 metabolism?
Naunyn Schmiedebergs Arch. Pharmacol.
377
205-207
2008
Rattus norvegicus
Kirino, Y.; Kamimoto, T.; Sato, Y.; Kawazoe, K.; Minakuchi, K.; Nakahori, Y.
Increased plasma dipeptidyl peptidase IV (DPP IV) activity and decreased DPP IV activity of visceral but not subcutaneous adipose tissue in impaired glucose tolerance rats induced by high-fat or high-sucrose diet
Biol. Pharm. Bull.
32
463-467
2009
Rattus norvegicus
Nordhoff, S.; Cerezo-Galvez, S.; Deppe, H.; Hill, O.; Lopez-Canet, M.; Rummey, C.; Thiemann, M.; Matassa, V.G.; Edwards, P.J.; Feurer, A.
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV
Bioorg. Med. Chem. Lett.
19
4201-4203
2009
Rattus norvegicus
Gupta, R.C.; Chhipa, L.; Mandhare, A.B.; Zambad, S.P.; Chauthaiwale, V.; Nadkarni, S.S.; Dutt, C.
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor
Bioorg. Med. Chem. Lett.
19
5021-5025
2009
Rattus norvegicus
Yeh, T.K.; Tsai, T.Y.; Hsu, T.; Cheng, J.H.; Chen, X.; Song, J.S.; Shy, H.S.; Chiou, M.C.; Chien, C.H.; Tseng, Y.J.; Huang, C.Y.; Yeh, K.C.; Huang, Y.L.; Huang, C.H.; Huang, Y.W.; Wang, M.H.; Tang, H.K.; Chao, Y.S.; Chen, C.T.; Jiaang, W.T.
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
Bioorg. Med. Chem. Lett.
20
3596-3600
2010
Homo sapiens, Rattus norvegicus
Krupina, N.A.; Kushnareva, E.Y.; Khlebnikova, N.N.; Zolotov, N.N.; Kryzhanovskii, G.N.
Behavioral changes in rats induced by a dipeptidyl peptidase IV inhibitor methionyl-2(S)-cyanopyrrolidine: experimental model of anxiety-depression disorder
Bull. Exp. Biol. Med.
147
285-290
2009
Rattus norvegicus
Luft, V.C.; Schmidt, M.I.; Pankow, J.S.; Hoogeveen, R.C.; Couper, D.; Heiss, G.; Duncan, B.B.; Duncan, B.B.
Dipeptidyl peptidase IV and incident diabetes: the Atherosclerosis Risk in Communities (ARIC) study
Diabetes Care
33
1109-1111
2010
Rattus norvegicus
Kiraly, K.; Szalay, B.; Szalai, J.; Barna, I.; Gyires, K.; Verbeken, M.; Ronai, A.Z.
Intrathecally injected Ile-Pro-Ile, an inhibitor of membrane ectoenzyme dipeptidyl peptidase IV, is antihyperalgesic in rats by switching the enzyme from hydrolase to synthase functional mode to generate endomorphin 2
Eur. J. Pharmacol.
620
21-26
2009
Rattus norvegicus
Hung, T.T.; Wu, J.Y.; Liu, J.F.; Cheng, H.C.
Epitope analysis of the rat dipeptidyl peptidase IV monoclonal antibody 6A3 that blocks pericellular fibronectin-mediated cancer cell adhesion
FEBS J.
276
6548-6559
2009
Rattus norvegicus (P14740)
Kirino, Y.; Sato, Y.; Kamimoto, T.; Kawazoe, K.; Minakuchi, K.; Nakahori, Y.
Interrelationship of dipeptidyl peptidase IV (DPP4) with the development of diabetes, dyslipidaemia and nephropathy: A streptozotocin-induced model using wild-type and DPP4-deficient rats
J. Endocrinol.
200
53-61
2009
Rattus norvegicus
Alponti, R.F.; Frezzatti, R.; Barone, J.M.; Alegre, V.D.; Silveira, P.F.
Dipeptidyl peptidase IV in the hypothalamus and hippocampus of monosodium glutamate obese and food-deprived rats
Metab. Clin. Exp.
60
234-242
2011
Rattus norvegicus (P14740)
Arscott, W.; LaBauve, A.; May, V.; Wesley, U.
Suppression of neuroblastoma growth by dipeptidyl peptidase IV: Relevance of chemokine regulation and caspase activation
Oncogene
28
479-491
2009
Rattus norvegicus
Ikuma, Y.; Hochigai, H.; Kimura, H.; Nunami, N.; Kobayashi, T.; Uchiyama, K.; Umezome, T.; Sakurai, Y.; Sawada, N.; Tadano, J.; Sugaru, E.; Ono, M.; Hirose, Y.; Nakahira, H.
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors: Use of a carboxylate prodrug to improve bioavailability
Bioorg. Med. Chem.
23
779-790
2015
Rattus norvegicus
Gomez, H.; Chappe, M.; Valiente, P.A.; Pons, T.; Chavez, M.d.e..L.; Charli, J.L.; Pascual, I.
Effect of zinc and calcium ions on the rat kidney membrane-bound form of dipeptidyl peptidase IV
J. Biosci.
38
461-469
2013
Rattus norvegicus
Rhnert, P.; Schmidt, W.; Emmerlich, P.; Goihl, A.; Wrenger, S.; Bank, U.; Nordhoff, K.; Tger, M.; Ansorge, S.; Reinhold, D.; Striggow, F.
Dipeptidyl peptidase IV, aminopeptidase N and DPIV/APN-like proteases in cerebral ischemia
J. Neuroinflammation
9
44
2012
Rattus norvegicus
EXTERNAL LINKS (specific for EC-Number 3.4.14.5)
Transporter Classification Database (TCDB): 8.A.51.1.5
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
