1235406-09-3
Chemical Structure
GX-936
Synonym(s): PF-05196233
- CAS No.: 1235406-09-3
- Formula:C24H20F3N7O3S2
- Molecular Weight:575.59
IUPAC Name: 3-cyano-4-(2-(1-(1-ethylazetidin-3-yl)-1H-pyrazol-5-yl)-4-(trifluoromethyl)phenoxy)-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide
InChIKey: UCAVSLIXTXZSRD-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(C(C#N)=C1)OC2=CC=C(C=C2C3=CC=NN3C4CN(C4)CC)C(F)(F)F)(NC5=NC=NS5)=O
Biological Activity: GX-936 (PF-05196233) is a selective Nav1.7 inhibitor. GX-936 binds to the activated VSD4, forms a bidentate salt bridge with the R4 of the S4 helix, traps VSD4 in the activated state, and prevents the channel from recovering from the inactivated state. GX-936 can be used in studies related to pain[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GX-936 | 97.06% | GX-936 (PF-05196233) is a selective Nav1.7 inhibitor. GX-936 binds to the activated VSD4, forms a bidentate salt bridge with the R4 of the S4 helix, traps VSD4 in the activated state, and prevents the channel from recovering from the inactivated state. GX-936 can be used in studies related to pain. | ||||||||||||||||||||
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References
- [1]. Storer RI, et al. Highly potent and selective Na1.7 inhibitors for use as intravenous agents and chemical probes. Bioorganic & medicinal chemistry letters. 2017 Nov 01;27(21):4805-4811. [Content Brief]
- [2]. Ahuja S, et al. Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist. Science. 2015 Dec 18;350(6267):aac5464. [Content Brief]
- [3]. Payandeh J, et al. Selective Ligands and Drug Discovery Targeting the Voltage-Gated Sodium Channel Nav1.7. Handbook of experimental pharmacology. 2018;246:271-306. [Content Brief]
