od1

Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases

m3-Huwentoxin IV (m3-HwTx-IV) is a potent inhibitor of sodium channels (NaV), with half-maximal inhibitory concentrations (IC50s) of 3.3 nM for hNaV1.7, 6.8 nM for hNaV1.6, 7.2 nM for hNaV1.3, 8.4 nM for hNaV1.1, 11.9 nM for hNaV1.2, and 369 nM for hNaV1.4 in the QPatch assay. It also alleviates spontaneous pain in a rodent model induced by the NaV1.7 activator OD1 in a dose-dependent manner [1].

Potent Nav1.7 blocker (IC50 = 2.5 nM). Also inhibits Nav1.1, Nav1.2, Nav1.3 and Nav1.6 in the nanomolar range. Exhibits no effects on Cav channels or nAChR at 5 μM. Demonstrates analgesic activity in vivo; antagonizes effects of scorpion-venom toxin OD1 a