ICA-121431
Nav1.1/1.3 inhibitor (selective) / Selective Nav1.1/1.3 inhibitor (hIC50s = 23 and 13 nM respectively; also selective for dog, monkey, and mouse, but not rat).1 It exclusively shifts voltage dependence to more negative voltages and accelerates entry into slow activation.2
Biochemicals & reagents
313254-51-2
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
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain