| Chemical Properties | Back Directory | [density ]
1.59±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 100 mg/mL (194.63 mM; Need ultrasonic) | [form ]
Solid | [pka]
8.67±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively[1]. Umibecestat can be used for the research of alzheimer's disease. | [in vivo]
Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows a dose-dependent effects on Aβ40 and a long duration of action in both rat brain and CSF[1].
Umibecestat (CNP520) (3.1 mg/kg; oral administration; 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]. | Animal Model: | Male rats (3-4 months old)[1] | | Dosage: | 1.5 mg/kg (3 μM/kg)-51.3 mg/kg (100 μM/kg) | | Administration: | Given by oral gavage; 72 hours | | Result: | Reduced 89.3±4.5% Aβ40 at the highest dose in brain tissue, and 50% lowering of rat brain Aβ40 (ED50) was 2.4±0.31 mg/kg. Reduced ~50% Aβ40 at a single oral 30 μM/kg (15.4 mg/kg) dose after 24 hours in both rat brain and CSF。 |
| Animal Model: | 3-month-old beagle dogs[1] | | Dosage: | 3.1 mg/kg (6 μM/kg) | | Administration: | Oral administration; 7 days | | Result: | Both Aβ40 and Aβ42 concentrations in CSF showed a > 75% reduction at 12-48 h after dosing and returned slowly to baseline over the next 7 days. |
| [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. DOI:10.15252/emmm.201809316 |
|
|