Sacubitril hemicalcium salt

  • Chemical Properties
CAS No. 1369773-39-6 Cat. No. BCP11897
Name Sacubitril hemicalcium salt
Synonyms LCZ696 hemicalcium salt; LCZ 696 hemicalcium salt; LCZ696 hemicalcium salt;AHU-377 hemicalcium salt;AHU377 hemicalcium salt;AHU 377 hemicalcium salt;
Formula 2(C24H28NO5).Ca M. Wt 861.04
  • Biological Activity
Description LCZ696 is a novel single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377 (1:1 ratio). Oral administration of LCZ696 caused dose-dependent increases in atrial natriuretic peptide immunoreactivity (due to NEP inhibition) in Sprague-Dawley rats 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) oral administration of LCZ696 showed that peak plasma concentrations were reached rapidly for valsartan (1.6-4.9 hours), AHU377 (0.5-1.1 hours), and its active moiety, LBQ657 (1.8-3.5 hours). LCZ696 is superior to valsartan alone in reducing blood pressure. Preliminary results from a Phase II trial showed that LCZ696 reduced NT-proBNP to a greater extent than valsartan alone, and in addition LCZ696 had beneficial effects on symptoms.
Pathways Protease/Metabolic Enzyme 
Targets Neprilysin 

Structure

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