GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7 , with an IC 50 of 3 nM.
In Vitro
GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC 50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Na v 1.7 3 nM (IC 50 )
Associated Targets(Human)
SCN2ATclinSodium channel protein type 2 subunit alpha (2 Activities)
