Azilsartan D5

An internal standard for the quantification of azilsartan

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1mg

￥2112.00

1690.00

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5mg

￥8850.00

7080.00

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货号: ajce55146
CAS: 1346599-45-8
别名: 阿齐沙坦D5; TAK-536-d5
分子式: C25H15D5N4O5
分子量: 461.48
纯度: >98%
溶解度: DMSO: slightly soluble,Methanol: slightly soluble
储存: Store at -20°C
库存: 现货

Background

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)