For research use only. Not for therapeutic Use.
GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7[1].
GX-201 has a relatively long half-life in mice[1].
GX-201 produces analgesia at a free plasma concentration about 3 times the IC50 for high-affinity channel block[1].
GX-201 inhibits nociceptive responses induced by formalin and inflammatory pain caused by complete Freund’s adjuvant (CFA)[1].
| Catalog Number | I028539 |
| CAS Number | 1788071-27-1 |
| Synonyms | 4-[[1-[[2-chloro-5-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamide |
| Molecular Formula | C25H27ClF4N2O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H27ClF4N2O4S/c1-37(34,35)31-24(33)20-11-19(16-2-3-16)23(12-22(20)27)36-14-15-6-8-32(9-7-15)13-17-10-18(25(28,29)30)4-5-21(17)26/h4-5,10-12,15-16H,2-3,6-9,13-14H2,1H3,(H,31,33) |
| InChIKey | KYBPOTYVFWNSGS-UHFFFAOYSA-N |
| SMILES | CS(=O)(=O)NC(=O)C1=C(C=C(C(=C1)C2CC2)OCC3CCN(CC3)CC4=C(C=CC(=C4)C(F)(F)F)Cl)F |
| Reference | [1]. Girish Bankar, et al. Selective Na V 1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain. Cell Rep. 2018 Sep 18;24(12):3133-3145. |
