Compounds > cgs 35601
Page last updated: 2024-11-12

cgs 35601

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

CGS 35601: a single molecule triple vasopeptidase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11464980
SCHEMBL ID489801
MeSH IDM0499455

Synonyms (15)

Synonym
cgs 35601
cgs-35601
1h-indole-3-propanoic acid, .alpha.-(((1-(((2s)-2-mercapto-4-methyl-1-oxopentyl)amino)cyclopentyl)carbonyl)amino)-, (.alpha.s)-
l-tryptophan, n-((1-(((2s)-2-mercapto-4-methyl-1-oxopentyl)amino)cyclopentyl)carbonyl)-
unii-7d7ks7y7jy
849066-09-7
1h-indole-3-propanoic acid, alpha-(((1-(((2s)-2-mercapto-4-methyl-1-oxopentyl)amino)cyclopentyl)carbonyl)amino)-, (alphas)-
7d7ks7y7jy ,
SCHEMBL489801
Q27268103
(1-((s)-2-mercapto-4-methylpentanamido)cyclopentane-1-carbonyl)-l-tryptophan
(2s)-3-(1h-indol-3-yl)-2-[[1-[[(2s)-4-methyl-2-sulfanylpentanoyl]amino]cyclopentanecarbonyl]amino]propanoic acid
(s)-3-(1h-indol-3-yl)-2-(1-((s)-2-mercapto-4-methylpentanamido)cyclopentanecarboxamido)propanoic acid
AKOS040746691
PD129904

Research Excerpts

Overview

CGS 35601 is a potent triple vasopeptidase inhibitor (VPI) of angiotensin-converting enzyme (ACE), neutral endopepticase (NEP), and endothelin converting enzyme-1 (ECE-1) The inhibitors have respective IC(50) values of 22, 2, and 55 nM.

ExcerptReferenceRelevance
"CGS 35601 is a potent triple inhibitor of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme. "( CGS 35601 and its orally active prodrug CGS 37808 as triple inhibitors of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme.
Beil, ME; Bruseo, CW; Firooznia, F; Jeng, AY; Savage, P; Trapani, AJ, 2004)		3.21
"CGS 35601 is a potent triple vasopeptidase inhibitor (VPI) of angiotensin-converting enzyme (ACE), neutral endopeptidase (NEP), and endothelin-converting enzyme (ECE). "( Triple vasopeptidase inhibition normalizes blood pressure in conscious, unrestrained, and spontaneously hypertensive rats.
Arsenault, D; Battistini, B; Beaudoin, M; Belleville, K; Benrezzak, O; Blouin, A; Cayer, J; Daull, P; Jeng, AY; Nantel, F; Pheng, LH; Sirois, P, 2005)		1.77
"CGS 35601 is a triple vasopeptidase inhibitor (VPI) of angiotensin-converting enzyme, neutral endopeptidase, and endothelin-converting enzyme-1 with respective IC50 values of 22, 2, and 55 nM. "( The first preclinical pharmacotoxicological safety assessment of CGS 35601, a triple vasopeptidase inhibitor, in chronically instrumented, conscious, and unrestrained spontaneously hypertensive rats.
Battistini, B; Beaudoin, M; Belleville, K; Benrezzak, O; Blouin, A; Cayer, J; Daull, P; Jeng, AY; Lepage, R; Nantel, F; Sirois, P, 2006)		2.01
"CGS 35601 is a triple vasopeptidase inhibitor (VPI) of angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), and endothelin (ET) converting enzyme-1 (ECE-1), with respective IC(50) values of 22, 2, and 55 nM. "( The hemodynamic and metabolic profiles of Zucker diabetic fatty rats treated with a single molecule triple vasopeptidase inhibitor, CGS 35601.
Battistini, B; Beaudoin, M; Belleville, K; Berthiaume, N; Blouin, A; Cayer, J; Daull, P; Gadbois, S; Jeng, AY; Nantel, F; Sirois, P, 2006)		1.98

Dosage Studied

ExcerptRelevanceReference
" It also increased plasma ANP immunoreactivity by 103% for up to 4 hours and inhibited the angiotensin I-induced pressor response by an average of 49% within the first 4 hours after the same dosing regimen."( CGS 35601 and its orally active prodrug CGS 37808 as triple inhibitors of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme.
Beil, ME; Bruseo, CW; Firooznia, F; Jeng, AY; Savage, P; Trapani, AJ, 2004)		1.77
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		2.0210amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		2.4220amino acid zwitterion;
angiotensin II		human metabolite
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		2.0210divalent inorganic anion;
phosphite ion
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		2.0210
benazepril
benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.		2.0210benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
cgs 35066
CGS 35066: an endothelin-converting enzyme-1 inhibitor; structure in first source		2.0210
atrial natriuretic factor
Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.		2.4220polypeptide
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		2.4220
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Pressure, High
[description not available]		03.6330
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		03.6330
Cardiac Failure
[description not available]		02.9410
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		02.9410
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		02.9410
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0310
Alloxan Diabetes
[description not available]		02.0310