Ambrisentan

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). It inhibits contraction of isolated rabbit aortic rings induced by endothelin-1 (ET-1, Cay-24127) by 43.23% when used at a concentration of 1 µM. Ambrisentan inhibits ET-1-induced contraction of human pulmonary and radial arteries in vitro (Kd = 0.042 and 0.11 µM, respectively). 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. Formulations containing ambrisentan have been used in the treatment of PAH.Formal Name: alphaS-[(4,6-dimethyl-2-pyrimidinyl)oxy]-beta-methoxy-beta-phenyl-benzenepropanoic acid. CAS Number: 177036-94-1. Molecular Formula: C22H22N2O4. Formula Weight: 378.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml, Ethanol: slightly soluble, Methanol: slightly soluble. SMILES: CC1=NC(O[C@H](C(O)=O)C(OC)(C2=CC=CC=C2)C3=CC=CC=C3)=NC(C)=C1. InChi Code: InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1. InChi Key: OUJTZYPIHDYQMC-LJQANCHMSA-N.