Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine -induced Ca 2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy [1].
In Vitro, Nav1.2-IN-2 (Compound 1) (0.1-10 μM; 15 min) potently suppresses spontaneous synchronized Ca2+ oscillation amplitude and frequency in primary cultured neocortical neurons with IC50 values of 0.38 μM and 0.88 μM, respectively[1]. Nav1.2-IN-2 (0.1-10 μM; 15 min) potently inhibits Veratridine-induced Ca2+ influx in primary cultured neocortical neurons with an IC50 of 1.89 μM[1]. Nav1.2-IN-2 exhibits state-dependent inhibition of Nav1.2 in transiently transfected HEK-293 cells, shifting steady-state inactivation hyperpolarization by 10.99 mV and inhibiting the inactivated state with an IC50 of 0.18 μM, while having no effect on steady-state activation[1].
References:
[1]. Xu J, et al. Aniline analogues as synchronized Ca 2+ oscillation modulators: structure-activity relationship and mechanism. Eur J Med Chem. 2026;301:118267.
In Vitro, Nav1.2-IN-2 (Compound 1) (0.1-10 μM; 15 min) potently suppresses spontaneous synchronized Ca2+ oscillation amplitude and frequency in primary cultured neocortical neurons with IC50 values of 0.38 μM and 0.88 μM, respectively[1]. Nav1.2-IN-2 (0.1-10 μM; 15 min) potently inhibits Veratridine-induced Ca2+ influx in primary cultured neocortical neurons with an IC50 of 1.89 μM[1]. Nav1.2-IN-2 exhibits state-dependent inhibition of Nav1.2 in transiently transfected HEK-293 cells, shifting steady-state inactivation hyperpolarization by 10.99 mV and inhibiting the inactivated state with an IC50 of 0.18 μM, while having no effect on steady-state activation[1].
References:
[1]. Xu J, et al. Aniline analogues as synchronized Ca 2+ oscillation modulators: structure-activity relationship and mechanism. Eur J Med Chem. 2026;301:118267.