Masitinib is a potent inhibitor of the tyrosine kinase receptor colony-stimulating factor 1R (CSF-1R) (IC50 = 90 nM). It is also an NLRP3 inflammasome activator. Masitinib additionally inhibits the proteolytic activity of SARS-CoV-2 main protease (Mpro) and blocks viral replication, as well as acting as a PDGFRα/β inhibitor.
In vivo
, Masitinib ameliorates cognitive impairment in transgenic mice model of Alzheimer's disease, and slows disease progression in a rat model of amyotrophic lateral sclerosis (ALS). Orally bioavailable.
Caractéristiques techniques
| Marque | Tocris Bioscience |
| Réf. B-LABO | BL-RE-125426 |
| Réf. fabricant | 18778176 |
| Nom chimique ou matériau | 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide |
|---|
| CAS | 790299-79-5 |
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| Quantité | 10 mg |
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| Cible | CD117/c-kit |
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| Formule moléculaire | C<sub>28</sub>H<sub>30</sub>N<sub>6</sub>OS |
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| Pureté | 0.98 |
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