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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).1 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.
WARNING This product is not for human or veterinary use.
1. Analgesic effects of GpTx-