Language
AHU-377的生物活性
AHU-377 is a potent neprilysin inhibitor.
IC50 Value: N/A
Target: neprilysin
in vitro: N/A
in vivo: 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). [1]. 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 [2].
化学信息
| 分子量 | 411.49 | 储存条件 | 参考CoA中推荐的条件进行储存。 |
|---|---|---|---|
| 分子式 | C24H29NO5 | ||
| CAS号 | 149709-62-6 | ||
| 溶剂/溶解度 | 10 mM in DMSO |
