Potent and selective inhibitor of the voltage gated sodium channel 1.7 (Nav1.7).1,3 It is a state-dependent inhibitor with IC50 = 11 nM for the half-inactivated channels and IC50 ~ 10 µM for resting channels.1 Equipotent for human, monkey, dog, and mouse channels but 15x less potent for rat channels. Interacts equally with fast and slow inactivated Nav1.7 channels.2
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