Sacubitril 是一种有效的NEP抑制剂，IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。

AHU-377 is a potent NEP inhibitor with an IC50 of 5 nM. AHU-377 is a component of the heart failure medicine LCZ696.

LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio). AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, AHU377, 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[3].

In humans, AHU377 (tmax?0.5-1.1 h) are absorbed quickly. AHU377 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[2].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 AHU377. Urinary volume is also potentiated in animals which receive an iv administration of AHU377[1].

149709-62-6

C24H29NO5

411.49

AHU 377;沙库必曲;AHU377;AHU-377

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years