Valsartan D9

Chemical Properties

White Solid

Uses

An isotopically labelled version of Valsartan (V095750), a nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.

Biological Activity

Valsartan-d9 is intended for use as an internal standard for the quantification of valsartan by GC- or LC-MS. Valsartan is a nonpeptide antagonist of the angiotensin II type 1 (AT1) receptor (IC50 = 2.7 nM). It is 20,000-fold selective for AT1 over AT2 and, unlike some other AT receptor antagonists, does not alter peroxisome proliferator-activated receptor γ (PPARγ) activity in vitro. In vivo, valsartan (30 mg/kg) increases cardiac output and reduces left ventricular fibrosis in a model of heart failure with reduced ejection fraction in mice with streptozotocin-induced diabetes. Formulations containing valsartan have been used in the treatment of hypertension and heart failure.