Literature summary for 3.4.14.5 extracted from

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 (2007), J. Med. Chem., 50, 6450-6453.

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Application

Application	Comment	Organism
medicine	8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione is a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. Potential for once-daily treatment of type 2 diabetics	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione	a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. Potential for once-daily treatment of type 2 diabetics	Homo sapiens
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	Canis lupus familiaris
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	Macaca mulatta
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	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Canis lupus familiaris	-	-	-
Homo sapiens	P27487	-	-
Macaca mulatta	-	-	-
Rattus norvegicus	-	Wistar rat	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
blood plasma	-	Rattus norvegicus	-
blood plasma	-	Canis lupus familiaris	-
blood plasma	-	Macaca mulatta	-
Caco-2 cell	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
DPP-4	-	Rattus norvegicus
DPP-4	-	Canis lupus familiaris
DPP-4	-	Macaca mulatta
DPP-4	-	Homo sapiens

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Release 2023.1 (January 2023)