Chemical Name: 4-[[1-[[2-Chloro-5-(trifluoromethyl)phenyl]methyl]-4-piperidinyl]methoxy]-5-cyclopropyl-2-fluoro-N-(methylsulfonyl)benzamide
Biological ActivityGX 201 is a potent and selective Nav1.7 blocker (IC50 = 3.2 nM). Exhibits 10x selectivity for Nav1.7 over Nav1.1, Nav1.2, and Nav1.6 channels. Displays prolonged residency time on the Nav1.7 channel. Chronic dosing increases compound potency ~10-fold and provides efficacy that persists after the compound has cleared from plasma. Suppresses neuropathic pain in a mouse diabetic neuropathy model. Analgesic.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Selective NaV1.7 antagonists with long residence time show improved efficacy against inflammatory and neuropathic pain.
Banker et al.
Cell Rep., 2018;24:3133
Insensitivity to pain upon adult-onset deletion of NaV1.7 or its blockade with selective inhibitors
Shields et al.
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