Sacubitrilat, namely LBQ-657, is an inhibitor of endopeptidase and effective for hypertension and heart failure. Sacubitrilat is one of the impurities of sacubitril.
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Sacubitrilat (LBQ657) is characterized by its specific stereochemistry, making it a potent inhibitor (5 nM) of the neutral endopeptidase (NEP) through a comprehensive network of interactions at the enzyme's active site[1].
体内研究
The pharmacokinetic profiles of Sacubitrilat (LBQ657) was assessed following single oral doses of LCZ696 at either 400 or 1200 mg under fasting conditions. Sacubitrilat showed corresponding Tmax values of 2.07 and 3.05 hours. The maximum concentration (Cmax) of Sacubitrilat increases dose-proportionally, whereas Sacubitril and Valsartan show less than proportional increases between the doses[2].
体外研究
Sacubitrilat (LBQ657) is characterized by its specific stereochemistry, making it a potent inhibitor (5 nM) of the neutral endopeptidase (NEP) through a comprehensive network of interactions at the enzyme's active site[1].
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