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GX-674 is a state-dependent inhibitor of voltage-gated sodium channel 1.7 (Nav1.7).1 It selectively inhibits Nav1.7 in HEK293 cells in a patch-clamp assay at -40 mV over -120 mV, voltages that correspond to steady-state inactivation and the resting closed state of the channel (IC50s = 0.1 and 240 nM, respectively). GX-674 is also selective for Nav1.7 over Nav1.1, Nav1.3-1.5, and Nav1.8 but does inhibit Nav1.2 and, to a lesser extent, Nav1.6.
WARNING This product is not for human or veterinary use.
1. Structural basis of Nav1.7 inhibition by an isoform-