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(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Ala-Pro
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(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Leu-Tyr
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-
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Phe-Ala
-
-
(2(R,S)-2-sulfanyl-2-benzyl)acetyl-Phe-Tyr
-
-
(2(R,S)-2-sulfanyl-2-isopropyl)acetyl-Ile-Tyr
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-
(2R)-2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
(2R)-2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-ethyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(4-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3,4-oxadiazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]-5-oxopentanoic acid
-
-
(2R)-2-[(1-[[(1S)-1-carboxy-2-(5-phenyl-1,3-oxazol-2-yl)ethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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-
(2R)-2-[[1-([(1S)-1-carboxy-2-[4-(2-methylpropyl)-1,3-oxazol-2-yl]ethyl]carbamoyl)cyclopentyl]methyl]pentanoic acid
-
-
(2R)-2-[[1-([(1S)-1-carboxy-2-[5-(4-chlorophenyl)-1,3-oxazol-2-yl]ethyl]carbamoyl)cyclopentyl]methyl]-5-oxopentanoic acid
-
-
(2R)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
-
(2S)-2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
(2S)-2-[(1-[[2-(hydroxymethyl)-2,3-dihydro-1H-inden-2-yl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
-
(2S)-2-[(1-[[3-(4-chlorophenyl)propyl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
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(2S)-2-[(1-[[3-(4-fluorophenyl)propyl]carbamoyl]cyclopentyl)methyl]-4-methoxybutanoic acid
-
-
(2S)-2-[[(2S)-1-[[(1S)-2-(biphenyl-4-yl)-1-carboxyethyl]amino]-5-methyl-1-oxohexan-2-yl]amino]-4-phenylbutanoic acid (non-preferred name)
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(2S)-4-methoxy-2-([1-[(1-methyl-2-phenylethyl)carbamoyl]cyclopentyl]methyl)butanoic acid
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(2S)-4-methoxy-2-[(1-[[(1R,2S)-2-(4-methoxyphenyl)cyclopropyl]carbamoyl]cyclopentyl)methyl]butanoic acid
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(2S)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
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(S)-N-[2-(phosphonomethylamino)-3-(4-biphenylyl)-propionyl]-3-aminopropionic acid
-
effects of neutral endopeptidase in acute inflammation in the lung are studied using a newly developed murine model of smoke and burn injury using NEP antagonist CGS-24592. Smoke and burn-induced lung injury and inflammation in mice pretreated with CGS-24592 is exacerbated, leading to more plasma extravasation and severe airway inflammation
2,3-Dimercaptopropan-1-ol
-
weak
2-(1-heptylcarbamoyl-cyclopentylmethyl)-4-methoxy-butyric acid tert-butyl ester
-
-
2-(4-bromobenzyl)-4-oxo-5-sulfanyl-6-[4-(2-sulfanylpropan-2-yl)phenyl]hexanoic acid
-
2-(4-bromobenzyl)-4-oxo-5-sulfanyl-6-[4-(3-sulfanylpentan-3-yl)phenyl]hexanoic acid
-
2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-4-oxo-6-[4-[piperidin-4-yl(sulfanyl)methyl]phenyl]-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-(butan-2-yl)phenyl]-1-(morpholin-4-yl)-5-sulfanylhexane-1,4-dione
-
2-(4-bromobenzyl)-6-[4-(butan-2-yl)phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[2,3-dihydro-1H-inden-2-yl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
-
2-(4-bromobenzyl)-6-[4-[cyclopentyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
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2-(biphenyl-4-ylmethyl)-4-oxo-6-[4-[piperidin-4-yl(sulfanyl)methyl]phenyl]-5-sulfanylhexanoic acid
-
2-(biphenyl-4-ylmethyl)-6-[4-[2,3-dihydro-1H-inden-2-yl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
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2-(biphenyl-4-ylmethyl)-6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
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2-(biphenyl-4-ylmethyl)-6-[4-[cyclopentyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanylhexanoic acid
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2-([1-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 1500 nM
2-([1-[(1-benzyl-2-hydroxyethyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
-
IC50: 384 nM
2-([1-[(1-benzyl-6-oxo-1,6-dihydropyridin-3-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 313 nM
2-([1-[(1-ethyl-1H-1,2,3-triazol-4-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 82 nM
2-([1-[(3-ethylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 1710 nM
2-([1-[(4-benzylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 96 nM
2-([1-[(4-butylpyridin-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 184 nM
2-([1-[(4-carbamoylcyclohexyl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 150 nM
2-([1-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 30 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-4-phenylbutanoic acid
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IC50: 46 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-5-methylhexanoic acid
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IC50: 120 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)hexanoic acid
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IC50: 84 nM
2-([1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 60 nM
2-([1-[(5-methyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 176 nM
2-([1-[(5-phenyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 283 nM
2-([1-[(6-methoxypyridazin-3-yl)carbamoyl]cyclopentyl]methyl)pentanoic acid
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IC50: 374 nM
2-([1-[5-(1-benzyl-6-oxo-1,6-dihydropyridin-3-yl)-1,3,4-oxadiazol-2-yl]cyclopentyl]methyl)pentanoic acid
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IC50: 1139 nM
2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoic acid
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2-benzyl-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoic acid
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2-methoxymethyl-3-[1-(trans-2-phenyl-cyclopropylcarbamoyl)-cyclopentyl]-propionic acid tert-butyl ester
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2-[(1-[[(1R)-1-phenylethyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 530 nM
2-[(1-[[(1R)-3-(dimethylcarbamoyl)cyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 297 nM
2-[(1-[[(1R,2R)-2-benzylcyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 195 nM
2-[(1-[[(1R,2S)-2-propylcyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 890 nM
2-[(1-[[(3R)-1-benzylpyrrolidin-3-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 1060 nM
2-[(1-[[(3R)-1-carbamoylpyrrolidin-3-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 213 nM
2-[(1-[[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 700 nM
2-[(1-[[1-(hydroxymethyl)cyclopentyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 1710 nM
2-[(1-[[2-(hydroxymethyl)-2,3-dihydro-1H-inden-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 96 nM
2-[(1-[[4-(dimethylcarbamoyl)cyclohexyl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 370 nM
2-[(1-[[5-(2-methylpropyl)-1,3,4-thiadiazol-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 124 nM
2-[(1-[[5-(cyclopropylmethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]cyclopentyl)methyl]pentanoic acid
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IC50: 38 nM
2-[(3-iodo-4-hydroxy)phenylmethyl]-4-N-[3-hydroxyamino-3-oxo-1(phenylmethyl)propyl]amino-4-oxobutanoic acid
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i.e. RB104, use of the inhibitor in detecting nanogram quantities of the enzyme by inhibitor gel electrophoresis
2-[(3-iodohydroxy)phenylmethyl]-4-N-[3-hydroxyamino-3-oxo-1-phenylmethylpropyl]-amino-4-oxobutanoic acid
-
i.e. RB104, highly selective and potent inhibitor
2-[1-(2-hydroxymethyl-indan-2-ylcarbamoyl)-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
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2-[1-(4-butyl-pyridin-2-ylcarbamoyl)-cyclopentylmethyl]-4-methoxybutyric acid benzyl ester
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2-[1-(5-ethyl-[1,3,4]thiadiazol-2-ylcarbamoyl)-cyclopentylmethyl]-pentanoic acid
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-
2-[1-[2-(trans-4-chlorophenyl)-cyclopropylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
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2-[1-[3-(4-chloro-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[1-[3-(4-fluoro-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-4-methoxy-butyric acid tert-butyl ester
-
-
2-[[1-(1,3,4-thiadiazol-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
-
IC50: 377 nM
2-[[1-(2,3-dihydro-1H-inden-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
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IC50: 313 nM
2-[[1-(5-benzyl-1,3,4-oxadiazol-2-yl)cyclopentyl]methyl]pentanoic acid
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IC50: 3100 nM
2-[[1-(pyridin-2-ylcarbamoyl)cyclopentyl]methyl]pentanoic acid
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IC50: 1500 nM
3-[1-[(5-ethyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]propanoic acid
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IC50: 237 nM
3-[1-[2-(trans-4-chlorophenyl)-cyclopropylcarbamoyl]-cyclopentyl]-2-methoxymethyl-propionic acid tert-butyl ester
-
-
4-hydroxy-nonenal
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intracellular neprilysin develops 4-hydroxy-nonenal adducts after 24 h of 4-hydroxy-nonenal treatment. 4-Hydroxy-nonenal-modified neprilysin shows decreased catalytic activity, which is associated with elevations in amyloid beta1-40 in SH-SY5Y and H4 APP695wt cells. Incubation of cells with amyloid beta1-42 also induces 4-hydroxy-nonenal adduction of neprilysin
4-methoxy-2-(1-phenethylcarbamoyl-cyclopentylmethyl)-butyric acid benzyl ester
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-
4-methoxy-2-[1-(3-phenyl-propylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-(trans-2-pentyl-cyclopropylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-(trans-2-phenyl-cyclopropylcarbamoyl)-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[(trans-2-(4-fluorophenyl)-cyclopropylcarbamoyl)]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[(trans-2-(4-methoxy-phenyl)-cyclopropylcarbamoyl)]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[2-(4-methoxy-phenoxy)-ethylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[2-(4-methoxy-phenyl)-ethylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
4-methoxy-2-[1-[3-(4-methoxy-phenyl)-propylcarbamoyl]-cyclopentylmethyl]-butyric acid tert-butyl ester
-
-
6-(biphenyl-4-yl)-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
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6-[4-[(1-acetylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[(1-benzoylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
-
6-[4-[(1-benzylpiperidin-4-yl)(sulfanyl)methyl]phenyl]-2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoic acid
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6-[4-[cyclohexyl(sulfanyl)methyl]phenyl]-4-oxo-5-sulfanyl-2-[4-(thiophen-3-yl)benzyl]hexanoic acid
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AHU-377
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LCZ696 comprises molecular moieties of valsartan, and of the NEP inhibitor prodrug AHU377 ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester) (1:1 molar ratio). Oral administration of LCZ696 causes dose-dependent increases in atrial natriuretic peptide immunoreactivity due to NEP inhibition in Sprague-Dawley rats and provides sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats
amyloid beta1-42
-
incubation of cells with amyloid beta1-42 induces 4-hydroxy-nonenal adduction of neprilysin. In an apparent compensatory response, amyloid beta-treated cells show increased neprilysin mRNA and protein expression. Despite elevations in neprilysin protein, the activity is significantly lower compared with the neprilysin protein level
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atrial natriuretic factor
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candoxatril
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treatment increases plasma atrial natriuretic peptide levels and leads to significantly higher levels of atrial tissue cyclic GMP as well as plasma cyclic GMP. Candoxatril suppresses the shortening of atrial effective refractory period and monophasic action potential duration in the rapid atrial pacing model
cis-4-[([1-[(2S)-2-carboxy-3-(2-methoxyethoxy)propyl]cyclopentyl]carbonyl)amino]cyclohexanecarboxylic acid
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-
diisopropyl fluorophosphate
-
-
DL-[N-(3-mercapto-2-benzylpropanoyl)]glycine
-
following neprilysin inhibition, islet amyloid deposition and beta-cell apoptosis increase by 54 and 75%, respectively
fasidotrilat
fasidotrilat interacts with the Arg664 of hNEP with more consistent bidentate hydrogen bonding and with the His658 with monodentate hydrogen bonding
Hg2+
0.001-0.05 mM, modifies the recombinant enzyme conformation, and highly reduces the enzyme activity. Hg2+ incubation increases NEP protein levels, but does not change NEP mRNA levels nor the levels of the amyloid intracellular domain peptide, a protein fragment with transcriptional activity. The Hg2+-induced inhibition of the enzyme activity may be mediated by a conformational change resulting in reduced amyloid beta1-42 degradation
Insulin B chain
inhibits the activity with substrate N-(4-carboxy-1-oxobutyl)-L-alanyl-L-alanyl-N-(4-methoxy-2-naphthalenyl)-L-phenylalaninamide
LCZ696
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LCZ696 is a dual-acting angiotensin II-receptor and neprilysin inhibitor (ARNI) in a single molecule: angiotensin-receptor blockade via its valsartan molecular moiety, and neprilysin inhibition via its AHU377 molecular moiety. In a randomized, double-blind, placebo-controlled, active comparator study it is shown that compared with valsartan, dual-acting LCZ696 provides complementary and fully additive reduction of blood pressure
MCB3937
bifunctional inhibitor of NEP and DPP-IV
MCB4241
bifunctional inhibitor of NEP and DPP-IV
N-(2-benzyl-3-sulfanylpropanoyl)glycine
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synthetic NEP inhibitor
N-(2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoyl)-L-alanine
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N-(2-benzyl-4-oxo-6-phenyl-5-sulfanylhexanoyl)-L-tryptophan
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N-([1-[(2S)-2-carboxy-3-[[N2-(methylsulfonyl)-L-lysyl]amino]propyl]cyclopentyl]carbonyl)-L-tyrosine
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-
N-phenethylphosphonyl-L-leucyl-L-tryptophan
N-[(2RS)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-Gly
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N-[(2S)-3-phenyl-2-(sulfanylmethyl)propanoyl]-L-tryptophan
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N-[1(R,S)-carboxy-2-phenylethyl]-Phe-p-aminobenzoate
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N-[2-(4-bromobenzyl)-4-oxo-5-phenyl-5-sulfanylpentanoyl]-L-alanine
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N-[2-(4-bromobenzyl)-4-oxo-5-sulfanylhexanoyl]-L-tryptophan
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N-[2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-alanine
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N-[2-(4-bromobenzyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-tryptophan
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N-[2-(4-bromobenzyl)-6-methyl-4-oxo-5-sulfanyloctanoyl]-L-alanine
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N-[2-(biphenyl-4-ylmethyl)-4-oxo-5-sulfanylhexanoyl]-L-alanine
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N-[2-(biphenyl-4-ylmethyl)-4-oxo-6-phenyl-5-sulfanylhexanoyl]-L-alanine
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N-[2-(biphenyl-4-ylmethyl)-6-methyl-4-oxo-5-sulfanyloctanoyl]-L-alanine
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N-[2-benzyl-6-(4-bromophenyl)-4-oxo-5-sulfanylhexanoyl]-L-leucine
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N-[5-fluoresceinyl]-N'-[6-(3-mercapto-2-benzyl-1-oxopropyl)amino-1-hexyl]thiocarbamide
-
the inhibitor is a very potent probe for detecting membrane-bound enzyme for biological studies or diagnostic applications. Particularly useful for detecting the membrane-bound enzyme by flow cytometry
N-[N-[1(5)-carboxy-3-(4-hydroxyphenyl)propyl]-(5)-phenylalanyl]-(5)-isoserine
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sacubitrilat
LBQ657, the inhibitor is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency. The catalytic zinc atom of NEP is ligated by the side chains of residues His583, His587, and Glu646 with the fourth coordination provided by the carboxylate oxygen adjacent to the P1 methyl of the compound, the backbone amide of LBQ657 forms H-bonding interactions with the side chains of Asn542 and Arg717. Enzyme active site binding structure, interaction, and inhibition mechanism, modelling, overview. All of the molecular interactions between LBQ657 and the enzyme are noncovalent, in line with a reversible inhibition mode
SCH48446
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i.e. the diiodo analog of N-[N-[1(5)-carboxy-3-(4-hydroxyphenyl)propyl]-(5)-phenylalanyl]-(5)-isoserine
sialorphin
-
opiorphin homologue inhibits NEP
tert-butyl 2-([1-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]cyclopentyl]methyl)-4-methoxybutanoate
-
-
tris(2-carboxyethyl)phosphine
TCEP, strong inhibition
U46619
a thromboxane mimetic
1,10-phenanthroline
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-
2-mercaptoethanol
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amyloid beta
-
amyloid beta reduces global DNA methylation whilst increasing neprilysin DNA methylation and further suppressing the neprilysin expression in mRNA and protein levels. Amyloid beta induces epigenetic effects, implying that DNA methylation may be part of a vicious cycle involving the reduction in neprilysin expression along with a resultant increase in amyloid beta accumulation, and that amyloiud beta may induce global DNA hypo-methylation
-
amyloid beta
-
infusion with amyloid beta(25-35) induces decrease of somatostatin-like immunoreactive content, somatostatin mRNA levels, phosphorylated-cAMP-response element binding protein CREB content and neprilysin levels
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candoxatrilat
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-
candoxatrilat
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application restores vagal reflex bradycardia in old rats to levels similar to those in young neutral endopeptidase inhibitor-treated rats
dithiothreitol
-
-
EDTA
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-
L-Cys
-
-
Leu5-enkephalin
-
-
Leu5-enkephalin
-
hydrolysis of succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide
Met5-enkephalin
-
-
Met5-enkephalin
-
hydrolysis of succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide
N-phenethylphosphonyl-L-leucyl-L-tryptophan
NPLT, synthesis of the phosphoramidon derivative with enhanced permeability into the skin that shows inability to inhibit type I and type IV collagenase, but inhibits fibroblast elastase
N-phenethylphosphonyl-L-leucyl-L-tryptophan
NPLT, synthesis of the phosphoramidon derivative with enhanced permeability into the skin that shows inability to inhibit type I and type IV collagenase, but inhibits fibroblast elastase
N-phenethylphosphonyl-L-leucyl-L-tryptophan
NPLT, synthesis of the phosphoramidon derivative with enhanced permeability into the skin that shows inability to inhibit type I and type IV collagenase, but inhibits fibroblast elastase
NaCl
-
brain enzyme; lung enzyme
NaCl
-
no inhibition of the enzyme from brain and kidney
phosphoramidon
-
-
phosphoramidon
a typical inhibitor for metalloproteinase
phosphoramidon
strong, consistent interactions with Arg664, Glu531 and His658 of hNEP
phosphoramidon
the inhibitor induces a dramatic increase in amyloid-beta peptide levels
phosphoramidon
a typical inhibitor for metalloproteinase
phosphoramidon
-
neprilysin inhibition potentiates substance P-mediated neutrophil oxygen radical production and may promote other inflammatory activities during magnesium deficiency. Magnesium deficiency plus treatment with phosphoramidon reduces neprilysin activity by 48%, phosphoramidon or magnesium deficiency alone only reduce its activity by 26% and 15%, respectively
phosphoramidon
-
the inhibitor induces a dramatic increase in amyloid-beta peptide levels
phosphoramidon
a typical inhibitor for metalloproteinase
phosphoramidon
-
synthetic NEP inhibitor
thiol
-
kidney enzyme; lung enzyme
thiol
-
intestine enzyme; kidney enzyme
thiorphan
-
-
thiorphan
complete inhibition
thiorphan
Arg49 and Arg664 act to support the ligand binding in NEP
thiorphan
the inhibitor induces a dramatic increase in amyloid-beta peptide levels
thiorphan
-
thiorphan eliminates proteolysis of the alpha-subunit
thiorphan
1 mM, completely blocks neutral endopeptidase activity
thiorphan
-
plasma and lung A-type natriuretic peptide levels in rats treated with lipopolysaccharide are significantly higher than those in the control group, but are significantly decreased by thiorphan administration. Natriuretic peptide receptor-A mRNA levels do not differ significantly among the groups. Natriuretic peptide receptor-C mRNA levels in animals treated with lipopolysaccharide plus thiorphan group are significantly higher than those in the other groups
thiorphan
-
the inhibitor induces a dramatic increase in amyloid-beta peptide levels
thiorphan
a NEP-specific inhibitor
thiorphan-NH2
-
-
valsartan
-
LCZ696 comprises molecular moieties of valsartan, and of the NEP inhibitor prodrug AHU377 ((2R,4S)-5-biphenyl-4-yl-5-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester) (1:1 molar ratio). Oral administration of healthy volunteers is associated with increases in plasma cGMP, renin concentration and activity, and angiotensin II, providing evidence for NEP inhibition and angiotensin receptor blockade
additional information
-
proteins derived from the Tat protein of HIV
-
additional information
-
both staurosporine-stimulated caspase-3 activation, p53 and neprilysin expression and activity are not affected by over-expression or depletion of presenilin complex component TMP21
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additional information
no inhibition by 4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione and 4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
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additional information
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no inhibition by 4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione and 4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
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additional information
desing of neprilysin inhibitors containing an alpha-mercaptoketone HSC(R1R2)CO group, as zinc ligand, substituted alpha-mercaptoketones are specific neprilysin inhibitors, optimization of the enzyme-inhibitor interactions within the S1 subsite, overview. Role of the size of the inhibitor which interacts with the S1, S1', or S2' domain of the enzyme and the nature of the substituents R1, and R2 of the mercaptoketone group in inhibitor potency. Introduction of a cyclohexyl chain in R1, R2 position and a (3-thiophen)benzyl group in position R3 yields to the most potent inhibitor of this series with a Ki value
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additional information
structure-activity relationship studies. No or poor inhibition by 4-(2-aminoethyl)benzylsulfonyl fluoride (AEBSF), and Nalpha-tosyl-l-lysyl chloromethylketone (TLCK), and iodoacetamide
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additional information
molecular docking studies, overview. For substrate and inhibitor binding, Arg664 and Zn697 are identified as the most conserved residues
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additional information
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molecular docking studies, overview. For substrate and inhibitor binding, Arg664 and Zn697 are identified as the most conserved residues
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additional information
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application of aldosterone, atrial natriuretic peptide, asymmetric dimethylarginine, and angiotensin peptides fail to cause down-regulation of renal neprilysin expression in vitro
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