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Sacubitril hemicalcium salt

CAS No. : 1369773-39-6

MCE 站：Sacubitril hemicalcium salt

产品活性：Sacubitril (AHU-377) hemicalcium salt 是有效的NEP抑制剂，IC₅₀值为5 nM。Sacubitril hemicalcium salt 是研究心力衰竭药物 LCZ696 的一个组分。

研究领域：Metabolic Enzyme/Protease

作用靶点：Neprilysin

In Vitro: Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril hemicalcium salt, a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, Sacubitril hemicalcium salt, 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.

In Vivo: In humans, Sacubitril (AHU-377)(t_max 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt is converted rapidly into LBQ657 with its t_max being reached in 1.9-3.5 h. Mean t_1/2 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 Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377).

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