| Company Name: |
InvivoChem |
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+1-708-310-1919 +1-13798911105 |
| Email: |
sales@invivochem.cn |
| Company Name: |
Energy Chemical |
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400-0056266 |
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Verubecestat Trifluoroacetate manufacturers
- Verubecestat TFA
-
- $1980.00
-
2026-07-15
- CAS:2095432-65-6
- Purity:
- Supply Ability: 10g
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| | Verubecestat Trifluoroacetate Basic information |
| Product Name: | Verubecestat Trifluoroacetate | | Synonyms: | Verubecestat Trifluoroacetate;Verubecestat (TFA);(R)-5-Fluoro-N-(4-fluoro-3-(3-imino-2,5-dimethyl-1,1-dioxido-1,2,4-thiadiazinan-5-yl)phenyl)picolinamide 2,2,2-trifluoroacetate | | CAS: | 2095432-65-6 | | MF: | C19H18F5N5O5S | | MW: | 523.44 | | EINECS: | | | Product Categories: | | | Mol File: | 2095432-65-6.mol |  |
| | Verubecestat Trifluoroacetate Chemical Properties |
| storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | DMSO: 81 mg/mL (154.75 mM);Ethanol: 5 mg/mL (9.55 mM) | | Water Solubility | Water: Insoluble |
| | Verubecestat Trifluoroacetate Usage And Synthesis |
| 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 |
| | Verubecestat Trifluoroacetate Preparation Products And Raw materials |
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