Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.

CYP2C9:0.17 μM (IC50), CYP3A4:0.077 μM (IC50)

Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ～1.1 %[1].

Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response[1]. .

Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1]. Animal Model: Rats[1]Dosage: 0~100 mpk Administration: I.p.; 1 hour Result: Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response. Animal Model: Mice[1]Dosage: 10~100 mpk Administration: I.p.; 2 days Result: Displayed a dose-dependent reduction of the pain response.