生物活性 | |||
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描述 | Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2]. Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.16mL 0.23mL 0.12mL |
5.81mL 1.16mL 0.58mL |
11.61mL 2.32mL 1.16mL |
参考文献 |
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