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Description: ICA-121431 is a potent, highly selective small molecule inhibitor of the human Nav1.3 and Nav1.1 voltage gated sodium channels with IC50 of 19 nM. It exhibit up to 1, 000-fold selectivity for human Nav1.3/Nav1.1 (ICA-121431, IC50, 19 nM) vs. other TTX-sensitive or resistant (i.e., Nav1.5) sodium channels, in other words, it has little or no activity against human Nav1.5 or Nav1.7 channels. Voltage-gated sodium channels initiate action potentials in brain neurons, and sodium channel blockers are used in therapy of epilepsy.
References: Proc Natl Acad Sci U S A. 2013 Jul 16; 110(29):E2724-32.
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