Raxatrigine (hydrochloride)

Raxatrigine is an inhibitor of voltage-gated sodium channels (Nav, IC50s = 22, 13, 23, 10, 84, 15, 32, and 6 µM for Nav1.1-Nav1.8 channels in a FLIPR membrane potential assay using HEK293 cells). Its activity is state-dependent at the Nav1.7 channel, with a nine-fold increase in potency for the open/inactivated state (IC50 = 6.3 µM) compared to the closed/resting state (IC50 = 54 µM). Raxatrigine (30 mg/kg, i.p.) decreases spontaneous pain behavior in an OD1 mouse pain model.Formal Name: (2S)-5R-[4-[(2-fluorophenyl)methoxy]phenyl]-2-pyrrolidinecarboxamide, monohydrochloride. CAS Number: 934240-31-0. Synonyms: BIIB074, CNV1014802, GSK1014802A, Vixotrigine. Molecular Formula: C18H19FN2O2 . HCl. Formula Weight: 350.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 229 nm. SMILES: FC1=CC=CC=C1COC2=CC=C([C@@H]3N[C@H](C(N)=O)CC3)C=C2.Cl. InChi Code: InChI=1S/C18H19FN2O2.ClH/c19-15-4-2-1-3-13(15)11-23-14-7-5-12(6-8-14)16-9-10-17(21-16)18(20)22,/h1-8,16-17,21H,9-11H2,(H2,20,22),1H/t16-,17+,/m1./s1. InChi Key: HEPUBAGOKRIZEO-PPPUBMIESA-N.