4-(2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide Molecular Weight: 500.35

Description

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

References

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