PF-05089771
Selective Nav1.7 channel blocker / 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
Biochemicals & reagents
1235403-62-9
PF771
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
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain; Inflammation