LCZ696中间体 T4200

Product Introduction
Bioactivity


英文名: Sacubitril hemicalcium salt

描述: Sacubitril hemicalcium salt (AHU377 calcium salt) 是一种有效的 NEP 抑制剂，IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。

体外活性: AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, AHU377, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy.

体内活性: In humans, AHU377 (tmax 0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax being reached in 1.9-3.5 h. Mean t1/2 values for the biologically active LBQ657 is 9.9-11.1 h.In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive AHU377.

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 54 mg/mL


关键字: Cluster of differentiation 10 | Neprilysin | AHU-377 | AHU377 | Sacubitril hemicalcium salt | NEP | inhibit | CD10 | Sacubitril hemicalcium | Sacubitril | Neutral endopeptidase | AHU 377 | AHU-377 hemicalcium | AHU377 calcium | Inhibitor

相关产品: Racecadotril | Phosphoramidon Disodium | Sacubitrilat | Thiorphan | Sacubitril | NEP-IN-1 | Sacubitril/Valsartan | LHW090-A7

相关库: Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Hypertension Compound Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途