Formulation: A crystalline solid
Formal Name: αS-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid
Purity: ≥98%
Formula Markup: C22H22N2O4
Formula Weight: 378,4
Shelf life (days): 1460
CAS Number: 177036-94-1
Notes: 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 in the treatment of PAH.
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