AHU-377 Hemicalcium is a potent Neprilysin inhibitor with an IC50 of 5 nM.
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Sacubitril hemicalcium salt 化学结构 CAS号：1369773-39-6
Sacubitril hemicalcium salt 3D分子结构 CAS号：1369773-39-6
Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2]. Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3].
体内研究
Sacubitril (AHU-377) demonstrates quick absorption in humans, with a tmax of 0.5-1.1 hours, and its conversion to LBQ657 happens swiftly, reaching its tmax in 1.9-3.5 hours. LBQ657's mean half-life ranges from 9.9 to 11.1 hours[2].
In studies with vehicle-treated dogs, Sacubitril (AHU-377) notably increased urinary sodium excretion and volume following intravenous administration, enhancing the diuretic response to ANF[1].
体外研究
Sacubitril (AHU-377) is a single-molecule drug composed of the molecular parts of Valsartan (ARB) and Sacubitril hemicalsalt (neprilysin inhibitor) (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of ethyl ester to LBQ657, an active metabolite that inhibits neprilysin [2].
Sacubitril hemicalcium salt is an inactive NEPi precursor, which does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. However, the active NEPi LBQ657 slightly reduces cardiac myocyte hypertrophy without affecting cardiac fibroblasts[3].
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