GNE-131 is a potent, selective inhibitor of sodium channel NaV1.7 with IC50 of 3 nM, >80-fold selectivity over the cardiac sodium channel NaV1.5.
GNE-131 demonstrates effects on mouse NaV1.7 using the Qube automated electrophysiology platform with IC50 of 7 nM.
GNE-131 shows significant reduction of nociceptive behavior on aconitine-induced pain in transgenic IEM mice, with up to 85% reduction at the 30 mg/kg dose and a plasma concentration of 2.8 uM.
