For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019277 |
| CAS Number | 1388651-30-6 |
| Synonyms | N-[3-[(4aS,5R,7aS)-2-amino-5-methyl-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-(difluoromethyl)pyrazine-2-carboxamide |
| Molecular Formula | C19H18F3N5O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C19H18F3N5O2S/c1-9-12-7-30-18(23)27-19(12,8-29-9)11-4-10(2-3-13(11)20)26-17(28)15-6-24-14(5-25-15)16(21)22/h2-6,9,12,16H,7-8H2,1H3,(H2,23,27)(H,26,28)/t9-,12-,19-/m1/s1 |
| InChIKey | AACUJFVOHGRMTR-DPXNYUHVSA-N |
| SMILES | CC1C2CSC(=NC2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(N=C4)C(F)F)F)N |
| 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. |
