Azilsartan (2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid) | 147403-03-0

name

azilsartan

chemical name

2-ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid

activity

potent angiotensin ii type 1 (at1) receptor inverse agonist (ic50 = 2.6 nm at the human at1 receptor). inhibits angiotensin ii-induced ip1 accumulation in cos-7 cells; decreases maximal contraction of rabbit aortic strips in a concentration-dependent manner (pd'2 = 9.9). antihypertensive; prevents vascular cell proliferation and expression of pai-1.

MW

456.45

Formula:

c25h20n4o5

Solubility:

soluble to 100 mm in dmso

Purity:

>98 %

Storage:

store at rt

CAS No:

147403-03-0

French et al (2011) The angiotensin receptor blocker, azilsartan medoxomil (TAK-491), suppresses vascular wall expression of plasminogen activator inhibitor type-I protein potentially facilitating the stabilization of atherosclerotic plaques. J.Cardiovasc.Pharmacol. 58 143. PMID: 21558880.

Kajiya et al (2011) Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J.Hypertens. 29 2476. PMID: 21986624.

Ojima et al (2011) In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J.Pharmacol.Exp.Ther. 336 801. PMID: 21123673.