GX 201

GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Inflammation/Immunology

GX-201 has a relatively long half-life in mice[1]. GX-201 produces analgesia at a free plasma concentration about 3 times the IC50 for high-affinity channel block[1]. GX-201 inhibits nociceptive responses induced by formalin and inflammatory pain caused by complete Freund’s adjuvant (CFA)[1]. Animal Model: Wild-Type Mice[1]. Dosage: 0.3, 1, 3 mg/kg. Administration: Orally, once. Result: Produced a dose-dependent inhibition of the nociceptive events.

[1]. Girish Bankar, et al. Selective Na V 1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain. Cell Rep. 2018 Sep 18;24(12):3133-3145.