UmibeceSTAT 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂，对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM，可用于阿尔茨海默病的研究。

Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease.

Umibecestat is a potent inhibitor of BACE-1 that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].

In both rat brain and CSF, Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows dose-dependent effects on Aβ40 and a long duration of action. Umibecestat (3.1 mg/kg; p.o.; 7 days) shows a >75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1].

1387560-01-1

C19H15ClF7N5O2

513.8

CNP520

DMSO:95 mg/mL (184.90 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years