Azilsartan-d5 is intended for use as an internal standard for the quantification of azilsartan by GC- or LC-MS. Azilsartan is an antagonist of the angiotensin II type 1 receptor (AT1; IC50 = 0.42 ?M) and the active metabolite of azilsartan medoxomil .1,2 Azilsartan is formed from azilsartan medoxomil by hydrolysis in the gastrointestinal tract and liver.3 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).2 It reduces the maximal contractile response induced by angiotensin II in isolated rabbit aortic strips (pD2 = 9.9).2 Azilsartan (100 ng/kg, i.v.) inhibits the angiotensin II-induced pressor response in conscious normotensive rats.1
1.Kohara, Y., Kubo, K., Imamiya, E., et al.Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteresJ. Med. Chem.39(26)5228-5235(1996) 2.Ojima, M., Igata, H., Tanaka, M., et al.In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studiesJ. Pharmacol. Exp. Ther.336(3)801-808(2011) 3.Clas, S.-D., Sanchez, R.I., and Nofsinger, R.Chemistry-enabled drug delivery (prodrugs): Recent progress and challengesDrug Discov. Today19(1)79-87(2014)