Azilsartan

Azilsartan is an antagonist of the angiotensin II type 1 receptor (AT1, IC50 = 0.42 µM) and the active metabolite of azilsartan medoxomil (Cay-23805). Azilsartan is formed from azilsartan medoxomil by hydrolysis in the gastrointestinal tract and liver. Azilsartan also acts as an inverse agonist, inhibiting angiotensin II-induced accumulation of inositol-1-phosphate in COS-7 cells expressing recombinant human AT1 (IC50 = 2.6 nM). It reduces the maximal contractile response induced by angiotensin II in isolated rabbit aortic strips (pD2 = 9.9). Azilsartan (100 ng/kg, i.v.) inhibits the angiotensin II-induced pressor response in conscious normotensive rats.Formal Name: 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid. CAS Number: 147403-03-0. Synonyms: TAK-536. Molecular Formula: C25H20N4O5. Formula Weight: 456.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 3 mg/ml, Ethanol: 0.1 mg/ml. SMILES: CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC3=CC=C(C4=C(C5=NOC(N5)=O)C=CC=C4)C=C3. InChi Code: InChI=1S/C25H20N4O5/c1-2-33-24-26-20-9-5-8-19(23(30)31)21(20)29(24)14-15-10-12-16(13-11-15)17-6-3-4-7-18(17)22-27-25(32)34-28-22/h3-13H,2,14H2,1H3,(H,30,31)(H,27,28,32). InChi Key: KGSXMPPBFPAXLY-UHFFFAOYSA-N.