A nonpeptide ET-A receptor antagonist (IC50s = 0.251

Ambrisentan – 5 mg

Brand:
Cayman
CAS:
177036-94-1
Storage:
-20
UN-No:
Non-Hazardous - /

Ambrisentan is a nonpeptide endothelin A (ETA) receptor antagonist (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively).{37346} It inhibits contraction of isolated rabbit aortic rings induced by endothelin-1 (ET-1; Item No. 24127) by 43.23% when used at a concentration of 1 µM.{37347} Ambrisentan inhibits ET-1-induced contraction of human pulmonary and radial arteries in vitro (Kd = 0.042 and 0.11 μM, respectively).{37348} In a rat model of neonatal hyperoxic lung injury, ambrisentan (20 mg/kg per day, s.c.) reduces pulmonary arterial hypertension (PAH) as well as decreases PAH-induced right ventricular hypertrophy (RVH) and peak RV pressure.{37349} Formulations containing ambrisentan have been used to treat PAH.  

 

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Description

A nonpeptide ET-A receptor antagonist (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively); inhibits ET-1-induced contraction of human pulmonary and radial arteries in vitro (Kd = 0.042 and 0.11 μM, respectively); decreases PAH, RVH, and RV peak pressure in a rat model of neonatal hyperoxic lung injury (20 mg/kg per day, s.c.)

Formal name: αS-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid

Synonyms: 

Molecular weight: 378.4

CAS: 177036-94-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Cardiovascular System|Vasculature|Vasodilation

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