| Description | Elenbecestat (E2609) is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease. |
| In vitro | E2609 has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.E2609 is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay. |
| In vivo | 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.E2609 displays the plasma half-life of 12-16 hours after once daily dosing. |
| Synonyms | E2609 |
| molecular weight | 437.44 |
| Molecular formula | C19H18F3N5O2S |
| CAS | 1388651-30-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 250 mg/mL (571.51 mM) |
| References | 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. |