PF-06456384 is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 (SCN9A; IC50 = 0.01, ﹤0.1, 75 nM against human, mouse, rat Nav1.7, respectively, by conventional patch clamp; human Nav1.7 IC50 = 0.58 nM by PatchExpress electrophysiology) with >300-fold selectivity over other human NaVs (IC50 = 3 nM/NaV1.2, 5.8 nM/NaV1.6, 75 nM/NaV1.7, 314 nM/NaV1.1, 1.45 µM/NaV1.4, 2.59 µM/NaV1.5, 6.44 µM/NaV1.3, 26 µM/NaV1.8).
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