Catalog Number: 5931
Chemical Name: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
Biological Activity
Potent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.
Technical Data
  • M.Wt:
    672.56
  • Formula:
    C18H12Cl2FN5O3S2.C7H8O3S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1430806-04-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.
    Cao et al.
    Sci.Transl.Med., 2016;8:335ra56
  2. Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release.
    Alexandrou et al.
    PLoS One, 2016;11:e0152405

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