1235403-62-9

PF-05089771 (1235403-62-9) is a potent and selective inhibitor of the voltage gated sodium channel 1.7 (Nav1.7).1,3? It is a state-dependent inhibitor with IC50 = 11 nM for the half-inactivated channels and IC50 ~ 10 μM for resting channels.1? Equipotent for human, monkey, dog, and mouse channels but 15x less potent for rat channels. Interacts equally with fast and slow inactivated Nav1.7 channels.2

PF 05089771 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].

Nav1.7

Alexandrou et al. (2016), ?Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release; PLoS One, 11 e0152405 Theile et al. (2016), The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels; Mol. Pharmacol., 90 540 Swain et al. (2017), 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(V)1.7; J. Med. Chem., 60 7029