Candesartan-d4 is intended for use as an internal standard for the quantification of candesartan by GC- or LC-MS. Candesartan is an antagonist of the angiotensin II type 1 (AT1) receptor (Kis = 0.17, 0.12, and 0.12 nM for human AT1, rat AT1A, and rat AT1B recombinant receptors, respectively) and an active metabolite of the prodrug candesartan cilexitil (Item No. 10489). It is selective for AT1 over AT2 receptors (Ki = 26,500 nM for the human recombinant AT2 receptor). It inhibits angiotensin II-induced contraction of isolated rabbit aortic strips and increases in blood pressure in rats following intravenous administration (ID50 = 0.033 mg/kg). Formulations containing candesartan have been used in the treatment of hypertension and heart failure.
