Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC50 of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease [1].
In Vivo, Nav1.7-IN-19 (150 mg/kg, p.o., daily for 3-7 days) significantly increases the mechanical withdrawal threshold (MWT) in SD rats with spinal nerve ligation pain model[1]. Nav1.7-IN-19 (200 mg/kg, p.o., daily for 14 days) shows no obvious toxic reactions in rats[1].
In Vitro, Nav1.7-IN-19 shows inhibition rates of 0.5%, 3.1%, and 24.6% at concentrations of 3, 10, and 30 μM respectively[1].
References:
[1]. Wu R, et al. Design, synthesis, structure-activity relationship (SAR) and analgesic effect studies of novel arylsulfonamides as selective Nav1.7 inhibitors. Eur J Med Chem. 2025 Dec 5;299:118069.
In Vivo, Nav1.7-IN-19 (150 mg/kg, p.o., daily for 3-7 days) significantly increases the mechanical withdrawal threshold (MWT) in SD rats with spinal nerve ligation pain model[1]. Nav1.7-IN-19 (200 mg/kg, p.o., daily for 14 days) shows no obvious toxic reactions in rats[1].
In Vitro, Nav1.7-IN-19 shows inhibition rates of 0.5%, 3.1%, and 24.6% at concentrations of 3, 10, and 30 μM respectively[1].
References:
[1]. Wu R, et al. Design, synthesis, structure-activity relationship (SAR) and analgesic effect studies of novel arylsulfonamides as selective Nav1.7 inhibitors. Eur J Med Chem. 2025 Dec 5;299:118069.