| Identification | Back Directory | [Name]
Benzenesulfonamide, 3-cyano-4-[2-[1-(1-ethyl-3-azetidinyl)-1H-pyrazol-5-yl]-4-(trifluoromethyl)phenoxy]-N-1,2,4-thiadiazol-5-yl- | [CAS]
1235406-09-3 | [Synonyms]
GX-936
PF05196233
PF-05196233
PF 05196233
Benzenesulfonamide, 3-cyano-4-[2-[1-(1-ethyl-3-azetidinyl)-1H-pyrazol-5-yl]-4-(trifluoromethyl)phenoxy]-N-1,2,4-thiadiazol-5-yl- | [Molecular Formula]
C24H20F3N7O3S2 | [MOL File]
1235406-09-3.mol | [Molecular Weight]
575.59 |
| Hazard Information | Back Directory | [Description]
GX-936, also known as PF-05196233, is a Nav1.7 inhibitor. GX-936 inhibit Nav1.7 through a voltage-sensor trapping mechanism, likely by stabilizing inactivated states of the channel. | [Uses]
GX-936 (PF-05196233), a potent and Nav1.7-subtype selective inhibitor, binds to the activated state of voltage-sensor domain IV (VSD4)[1][2][3]. | [References]
[1] R Ian Storer, et al. Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4805-4811. DOI:10.1016/j.bmcl.2017.09.056
[2] Shivani Ahuja, et al. Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist. Science. 2015 Dec 18;350(6267):aac5464. DOI:10.1126/science.aac5464
[3] Jian Payandeh, et al. Selective Ligands and Drug Discovery Targeting the Voltage-Gated Sodium Channel Nav1.7. Handb Exp Pharmacol. 2018:246:271-306. DOI:10.1007/164_2018_97 |
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