Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
IC50&Target
BACE-1
体外研究
Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay.
Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.
体内研究
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.
Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing.
Animal Model:
Cynomolgus monkeys (Pharmacokinetic analysis)
Dosage:
0.3 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg
Administration:
Oral administration
Result:
Potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF.
分子式
C19H18F3N5O2S
分子量
437.44
CAS号
1388651-30-6
运输条件
Room temperature in continental US; may vary elsewhere.