An AT1 receptor antagonist (IC50 = 2.7 nM); 20

Valsartan – 100 mg

Brand:
Cayman
CAS:
137862-53-4
Storage:
-20
UN-No:
Non-Hazardous - /

Angiotensin II is a peptide hormone which regulates blood pressure and fluid balance, contributing to hypertension, atherosclerosis, left ventricular hypertrophy, myocardial infarction, and heart failure.{20935} Valsartan is a nonpeptide angiotensin II receptor antagonist of the angiotensin II type 1 (AT1) receptor (IC50 = 2.7 nM).{21001} It is 20,000-fold selective for AT1 over AT2 and, unlike some other AT receptor antagonists, does not alter peroxisome proliferator-activated receptor γ (PPARγ) activity in vitro.{20999} In vivo, valsartan (30 mg/kg) increases cardiac output and reduces left ventricular fibrosis in a model of heart failure with reduced ejection fraction in mice with streptozotocin-induced diabetes.{42153} Formulations containing valsartan have been used in the treatment of hypertension and heart failure.{20999,13660,12999}  

 

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Description

An AT1 receptor antagonist (IC50 = 2.7 nM); 20,000-fold selective for AT1 over AT2; does not alter PPARγ activity in vitro; increases cardiac output and reduces left ventricular fibrosis in a model of heart failure with reduced ejection fraction in mice with streptozotocin-induced diabetes at 30 mg/kg ,

Formal name: N-(1-oxopentyl)-N-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine

Synonyms:  CGP 48933

Molecular weight: 435.5

CAS: 137862-53-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension

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