GX 201 is a potent and selective Nav1.7 blocker (IC50 = 3.2 nM). Exhibits 10x selectivity for Nav1.7 over Nav1.1, Nav1.2, and Nav1.6 channels. Displays prolonged residency time on the Nav1.7 channel. Chronic dosing increases compound potency ∽10-fold and provides efficacy that persists after the compound has cleared from plasma. Suppresses neuropathic pain in a mouse diabetic neuropathy model. Analgesic.
Caractéristiques techniques
| Marque | Tocris |
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| Réf. B-LABO | BL-RE-124771 |
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| Réf. fabricant | 18727476 |
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| Nom chimique ou matériau | 4-[[1-[[2-Chloro-5-(trifluoromethyl)phenyl]methyl]-4-piperidinyl]methoxy]-5-cyclopropyl-2-fluoro-N-(methylsulfonyl)benzamide |
|---|
| CAS | 1788071-27-1 |
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| Quantité | 10 mg |
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| Cible | Voltage-gated Sodium Channel Blockers |
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| Formule moléculaire | C<sub>25</sub>H<sub>27</sub>ClF<sub>4</sub>N<sub>2</sub>O<sub>4</sub>S |
|---|
| Pureté | 0.98 |
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