| Bioactivity | 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]. | ||||||||||||
| Target | BACE-1 | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | Elenbecestat | ||||||||||||
| CAS | 1388651-30-6 | ||||||||||||
| Formula | C19H18F3N5O2S | ||||||||||||
| Molar Mass | 437.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Elenbecestat
CAS: 1388651-30-6 F: C19H18F3N5O2S W: 437.44
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential
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