An internal standard for the quantification of aliskiren
Aliskiren-d6 is intended for use as an internal standard for the quantification of aliskiren by GC- or LC-MS. Aliskiren is a nonpeptide inhibitor of renin (IC50 = 0.6 nM for the human enzyme).1 Aliskiren (10 and 30 mg/kg per day) reduces blood pressure and prevents albuminuria in renin-overexpressing TG(mRen-2)27 rats in a model of streptozotocin-induced diabetes.2 It also reduces cardiac hypertrophy and fibrosis induced by heart pressure overload in mice.3 Formulations containing aliskiren have been used in the treatment of hypertension.
1.Rhuel, R., Rasetti, V., Maibaum, J., et al.Structure-based drug design: The discovery of novel nonpeptide orally active inhibitors of human reninChem. Biol.7(7)493-504(2000) 2.Feldman, D.L., Jin, L., Xuan, H., et al.Effects of aliskiren on blood pressure, albuminuria, and (pro)renin receptor expression in diabetic TG(mRen-2)27 ratsHypertension52(1)130-136(2008) 3.Weng, L., Zhang, W., Ye, Y., et al.Aliskiren ameliorates pressure overload-induced heart hypertrophy and fibrosis in miceActa Pharmacol. Sin.35(8)1005-1014(2014)
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