Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :AHU-377 hemicalcium salt1369773-39-6HY-107A410.48C24H28NO5->98%Solubility:DMSOMechanisms: Pathways:Others; Target:Neprilysin Biological Activity:AHU377 hemicalcium salt is a potent neprilysin inhibitor with IC50 of 5.0 nM; a component ofAHU-377hemicalciumsaltisapotentneprilysininhibitorwithIC50of50nM;acomponentofLCZ696. IC50 Value: 5.0 nM Target: neprilysin in vitro: in vivo: LCZ696 is a novel single molecule comprising molecular moieties of valsartan and NEPinhibitor prodrug AHU377 (1:1 ratio). Oral administration of LCZ696 caused dose-dependentincreases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawleyrats and provided sustained, dose-dependent blood pressure reductions in hypertensive double-transgenic rats. In healthy participants, a randomized, double-blind, placebo-controlled study (n =80) of single-dose (200-1200 mg) and multiple-dose (50-900 mg once daily for 14 days) oraladministration of LCZ696 showed that peak plasma concentrations were reached rapidly forvalsartan (1.6-4.9 hours), AHU377 (0.5-1.1 hours), and its active moiety,...References:[1]. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem.1995M1238(10)16700 1995 May 12;38(10):16-700.[2]. Voors, A.A., B. Dorhout, and P. van der Meer, The potential role of valsartan + AHU377 (LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs, 2013. 22(8): p. 1041-7. [3]. Gu, J., et al., Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-actingangiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol, 2010. 50(4): p. 401-14. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 080,USAEmail: info@medchemexpress.com Web: www.medchemexpress.com
