ICA604025 is a state-dependent inhibitor of human Nav1.9 voltage-gated sodium channel. ICA604025 exerts stronger inhibitory effects on activated/inactivated Nav1.9 than on resting closed Nav1.9, and serves as a tool for investigating the physiological functions of Nav1.9. ICA604025 is applicable to pain-related research [1] [2].
In Vitro, ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits human Nav1.9-5C channels in HEK-293 cells, with an EC50 of 9 nM for activated/inactivated states and 1.1 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits wild-type human Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.76 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits cynomolgus monkey Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.45 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits mouse Nav1.9 channels in HEK-293 cells with an EC50 of 0.48 μM for activated/inactivated states, showing ~48-fold lower potency than for human Nav1.9[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits rat Nav1.9 channels in HEK-293 cells with an EC50 of 0.53 μM for activated/inactivated states, showing ~53-fold lower potency than for human Nav1.9[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits human Nav1.9-5CF1592A/Y1599A mutant channels in HEK-293 cells with an EC50 of 0.017 μM for activated/inactivated states, showing only a minor reduction in potency compared to wild-type Nav1.9-5C[1]. ICA604025 (0-10 μM) potently inhibits native Nav1.9 channels in human DRG neurons with an IC50 of 0.56 μM[2].
References:
[1]. Potet F, et al. Identification and characterization of selective inhibitors of Nav1.9 voltage dependent sodium channels. Molecular pharmacology. 2026;108(5-6):100125.
[2]. Shi YP, et al. Biophysical Characterization of the human Nav1.9 sodium channel in trigeminal ganglia and dorsal root ganglia neurons. bioRxiv. 2026 Aug 25.
In Vitro, ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits human Nav1.9-5C channels in HEK-293 cells, with an EC50 of 9 nM for activated/inactivated states and 1.1 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits wild-type human Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.76 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) potently and state-dependently inhibits cynomolgus monkey Nav1.9 channels in HEK-293 cells, with an EC50 of 10 nM for activated/inactivated states and 0.45 μM for resting closed states[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits mouse Nav1.9 channels in HEK-293 cells with an EC50 of 0.48 μM for activated/inactivated states, showing ~48-fold lower potency than for human Nav1.9[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits rat Nav1.9 channels in HEK-293 cells with an EC50 of 0.53 μM for activated/inactivated states, showing ~53-fold lower potency than for human Nav1.9[1]. ICA604025 (0.001-100 μM; 4 minutes) inhibits human Nav1.9-5CF1592A/Y1599A mutant channels in HEK-293 cells with an EC50 of 0.017 μM for activated/inactivated states, showing only a minor reduction in potency compared to wild-type Nav1.9-5C[1]. ICA604025 (0-10 μM) potently inhibits native Nav1.9 channels in human DRG neurons with an IC50 of 0.56 μM[2].
References:
[1]. Potet F, et al. Identification and characterization of selective inhibitors of Nav1.9 voltage dependent sodium channels. Molecular pharmacology. 2026;108(5-6):100125.
[2]. Shi YP, et al. Biophysical Characterization of the human Nav1.9 sodium channel in trigeminal ganglia and dorsal root ganglia neurons. bioRxiv. 2026 Aug 25.