Elenbecestat (E2609) 是一种高效、有口服活性的，能透过 CNS 的 BACE-1 抑制剂。Elenbecestat 有潜力用于阿尔茨海默病 (AD) 的研究。
货号:ajcx38652
CAS:1388651-30-6
分子式:C19H18F3N5O2S
分子量：437.44
溶解度:DMSO : ≥ 250 mg/mL (571.51 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research[1][2].

Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay[2].Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents[2].

Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates[2].Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing[1].

[1]. Kumar D, et al.Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead. Eur J Med Chem. 2018 Mar 25;148:436-452.
[2]. A single dose of the beta-secretase inhibitor, e2609, decreases CSF bace1 enzymatic activity in cynomolgus monkeys. Alzheimer's & Dementia, 8(4), P224.