PF 05089771 tosylate_product_DataBase

Bioactivity	PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7,ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy[1][2].
Target	IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7).
Invitro	PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4)[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].
Name	PF 05089771 tosylate
CAS	1430806-04-4
Formula	C25H20Cl2FN5O6S3
Molar Mass	672.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

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