A-803467

Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel with high activation threshold and slow inactivating kinetics that is highly expressed in small-diameter sensory neurons and has been implicated in signaling various types of pain. A-803467 is a sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8 sodium channels (IC50 = 8 nM when stimulated at half-maximal inactivation and IC50 = 79 nM at a resting state). This compound is unusual in that it blocks hNav1.8 at negative resting membrane potentials (many small molecule sodium channel blockers show a reduced affinity for the resting state) and does not demonstrate significant frequency-dependent block during a 10 Hz pulse train. A-803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.Formal Name: 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide. CAS Number: 944261-79-4. Molecular Formula: C19H16ClNO4. Formula Weight: 357.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 2.5 mg/ml. lambdamax: 319 nm. SMILES: COc1cc(OC)cc(c1)NC(=O)c1ccc(o1)c1ccc(Cl)cc1. InChi Code: InChI=1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22). InChi Key: VHKBTPQDHDSBSP-UHFFFAOYSA-N.