313254-51-2

ICA 121431 is a voltage-gated sodium channel (Na_v) blocker that selectively blocks Na_v1.1 and Na_v1.3 over Na_v1.4, and Na_v1.5-1.8 channels (IC₅₀s = <20, 19, 240, and >10,000 nM, respectively). It induces a concentration-dependent hyperpolarizing shift in voltage dependence of inactivation of Na_v1.3 channels at a concentration 1 μM but has no effect on resting channels. Substitution of the Na_v1.3 domain IV voltage-sensor domain (VSD4) with the Na_v1.5 VSD4 reduces ICA 121431 potency by approximately 500-fold.

ICA 121431 is a voltage-gated sodium (Nav) channel inhibitor.

hNa_v1.1: 13 nM (IC₅₀); hNa_v1.3: 23 nM (IC₅₀); hNa_v1.4: 240 nM (IC₅₀); hNa_v1.6: >10 μM (IC₅₀); hNa_v1.5: >10 μM (IC₅₀); hNa_v1.8: >10 μM (IC₅₀)

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McCormack et al. (2013), Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels; Proc. Natl. Acad. Sci. USA 110 E2724 Ostenn et al. (2017), Pharmacology of the Nav1.1 domain IV voltage sensor reveals coupling between inactivation gating processes; Proc. Natl. Acad. Sci. USA 114 6836