PF 05089771

Biological Activity

PF 05089771 is a potent and selective Na_v1.7 channel blocker (IC₅₀ = 8, 11 and 171 nM for mouse, human and rat Na_v1.7, respectively). Exhibits selectivity for Na_v1.7 over other Na_v1 channels (IC₅₀ values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Na_v1.2, Na_v1.6, Na_v1.1, Na_v1.4, Na_v1.3 and Na_v1.5, 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

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.

Additional Information

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 Na_v1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release.
   Alexandrou et al.
   PLoS One, 2016;11:e0152405
3. Discovery of clinical candidate 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): design and optimization of diaryl ether aryl sulfonamides as selective inhibitors of Na
   Swain et al.
   J.Med.Chem., 2017;60:7029

Product Datasheets