沙库比曲钙盐
| CAS号 | 1369773-39-6 | 货号 | BCP11897 |
| 中文名 | 沙库比曲钙盐 | ||
| 英文名 | Sacubitril hemicalcium salt | ||
| 中文别名 | |||
| 英文别名 | LCZ696 hemicalcium salt; LCZ 696 hemicalcium salt; LCZ696 hemicalcium salt;AHU-377 hemicalcium salt;AHU377 hemicalcium salt;AHU 377 hemicalcium salt; | ||
| 分子式 | 2(C24H28NO5).Ca | 分子量 | 861.04 |
| 生物活性 | 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. | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | Neprilysin | ||
结构式
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