化合物Sacubitrilat TQ0106

Product Introduction
Bioactivity


英文名: Sacubitrilat

描述: Sacubitrilat (LBQ-657) 是活性的脑啡肽酶 (NEP) 抑制剂。

体外活性: Sacubitrilat is bound to the active site of NEP by an intricate network of interactions that involves all functional groups of the compound giving rise to the high inhibitory potency of 5?nM [1].

体内活性: Pharmacokinetics of Sacubitril, Sacubitrilat, and valsartan following the administration of single oral doses of LCZ696 400 or 1200 mg under fasting conditions are summarized. The mean plasma concentrations of Sacubitril increases rapidly with a median Tmax of 0.52 h for the 400 mg dose and 1.05 h for the 1200 mg dose, followed by Sacubitrilat, with the corresponding Tmax values of 2.07 and 3.05 h, respectively. The median Tmax for valsartan is 2.07 h for both the LCZ696 400 mg and 1200 mg doses. The Cmax of Sacubitrilat shows a dose-proportional increase, while the Cmax of Sacubitril and Valsartan shows less than proportional increases between the doses [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (260.80 mM)


关键字: Desethyl Sacubitril | NEP | Neutral endopeptidase | Neprilysin | Inhibitor | inhibit | LBQ657 | LBQ 657 | CD10 | Cluster of differentiation 10 | Sacubitrilat

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

相关库: ReFRAME Related Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Inhibitor Library | Metabolism Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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