| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: 81 mg/mL (154.75 mM);Ethanol: 5 mg/mL (9.55 mM) | [Water Solubility ]
Water: Insoluble |
| Hazard Information | Back Directory | [Uses]
Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease[1][2]. | [Biological Activity]
Verubecestat (MK-8931) Trifluoroacetat is a potent and selective beta-secretase inhibitor, a BACE1 inhibitor. | [in vitro]
Verubecestat(MK-8931) effectively reduces Aβ40 in cells, Ki：7.8 nM and IC50 ：13 nM. | [in vivo]
single oral dose of Verubecestat (MK-8931) to rats and cynomolgus monkeys significantly reduced cerebrospinal fluid (CSF) and cortical Aβ40. MK-8931 has an in vivo half-life of 20 hours, and is suitable for a once-daily dosing frequency. | [target]
| Target | Value | BACE2
(Cell-free assay) | 0.37 nM(Ki) | BACE1
(Cell-free assay) | 1.75 nM(Ki) |
| [References]
[1] Yan R, et al. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13. DOI:10.1186/s40035-016-0061-5
[2] Scott JD, et al. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer'sDisease. Med Chem. 2016 Dec 8;59(23):10435-10450. DOI:10.1021/acs.jmedchem.6b00307 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
A.J Chemicals
|
| Tel: |
91-9810153283 |
| Website: |
www.ajchemicals.com |
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