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Sacubitril hemicalcium salt
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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)(tmax 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt 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 Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377).
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Sacubitril | Sacubitrilat | Phosphoramidon Disodium | Racecadotril | Sampatrilat | SCH 42495 racemate | Candoxatril | NEP-In-1 | NEP-IN-2 | SQ28603
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热门标签:AHU-377 hemicalcium salt