Sacubitrilat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sacubitrilat (LBQ657) 是活性脑啡肽酶 (NEP) 的有效抑制剂。Sacubitrilat 通过复杂的相互作用网络与 NEP 的活性位点结合，该网络涉及化合物的所有官能团，从而产生 5 的高抑制效力纳米。

Sacubitrilat (LBQ657) is an effective inhibitor of active neprilysin (NEP).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.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.

——

——

LBQ-657

Metabolic Enzyme/Protease

Neprilysin

Neprilysin

——

——

149709-44-4

383.44

C22H23NO5

>98% (HPLC)

DMSO:100 mg/mL (260.80 mM)

[H]N(C(CCC(O)=O)=O)[C@H](CC(C=C1)=CC=C1C2=CC=CC=C2)C[C@H](C(O)=O)C

——

(-20℃)

With Ice Pack

≥ 2 years