ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Na v ) blocker, shows equipotent selectivity for human Na v 1.1 and Na v 1.3 subtypes with IC 50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na v 1.2 ( IC 50 =240 nM) and 1,000 fold selectivity against Na v 1.4, Na v 1.6, and the TTX-resistant human Na v 1.5 and Na v 1.8 channels ( IC 50 s >10 μM).
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