Umibecestat (CNP520) 是一种 β 位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂， 在人 BACE-1 和鼠 BACE-1 中的 IC50 值分别为 11 nM 和 10 nM。Umibecestat 可用于阿尔茨海默病的研究。
货号:ajcx39432
CAS:1387560-01-1
分子式:C19H15ClF7N5O2
分子量：513.8
溶解度:DMSO : 100 mg/mL (194.63 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively[1]. Umibecestat can be used for the research of alzheimer's disease.

Umibecestat (CNP520) is a potent BACE-1 inhibitor that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1].

Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF[1].Umibecestat (CNP520) (3.1 mg/kg; oral administration; 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].

[1]. Neumann U, et al. The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. EMBO Mol Med. 2018 Nov;10(11). pii: e9316.