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基本信息
沙库巴曲钙
沙库必曲钙盐
沙库巴曲钙盐
LCZ中间体
沙库比曲钙盐
HU377钙盐
AHU377钙盐
原研534-06
LCZ696杂质P
LCZ696-1
Sacubitril Calcium
AHU377 Calcium Salt
AHU-377 Hemicalcium
LCZ696 Impurity 534-06
Sacubitril calcium salt
AHU-377 (heMicalciuM salt)
Sacubitril Hemicalcium salt
AHU-377 hemicalcium salt (2:1)
物理化学性质
安全数据
常见问题列表
沙必利是一种与缬沙坦联合使用的降压药。这种名为缬沙坦/沙必利的联合药物在试验中被称为LCZ696,并以Entresto品牌销售,是一种治疗心力衰竭的药物。本品用作该药物中间体和杂质对照品,用于药品申报检测等。
IC50: 5 nM (NEP)
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 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).