PF 05089771 tosylate 

PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor, with IC₅₀ values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy^[1][2].

IC50: 11 nM (hNa_v1.7), 12 nM (cynNa_v1.7), 13 nM (dogNa_v1.7), 171 nM (ratNa_v1.7), 8 nM (musNa_v1.7)^[1][2].

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Na_v1.2 to 900-fold for Na_v1.3 and Na_v1.4)^[1].
PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5) whilst 100 nM resulted in complete block^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

672.56

C₂₅H₂₀Cl₂FN₅O₆S₃

1430806-04-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405.  [Content Brief]

  [2]. Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548.  [Content Brief]