| Description | Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease. |
| In vitro | Umibecestat is a potent inhibitor of BACE-1 that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1]. |
| In vivo | In both rat brain and CSF, Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows dose-dependent effects on Aβ40 and a long duration of action. Umibecestat (3.1 mg/kg; p.o.; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1]. |
| Target activity | BACE1 (human):11 nM , BACE1 (mouse):10 nM |
| Synonyms | CNP520 |
| molecular weight | 513.8 |
| Molecular formula | C19H15ClF7N5O2 |
| CAS | 1387560-01-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95 mg/mL (184.90 mM), Sonication is recommended. |
| References | 1. Neumann U, et al. The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. EMBO Mol Med. 2018 Nov;10(11). pii: e9316. |