Chemical Name: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
Biological ActivityPotent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.
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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
Swain et al.
Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.
Cao et al.
Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release.
Alexandrou et al.
PLoS One, 2016;11:e0152405
Citation for PF 05089771
The citations listed below are publications that use Tocris products. Selected citations for PF 05089771 include:
1 Citation: Showing 1 - 1
The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes.
Authors: Cheng Et al.
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The effect of PF-05089771, a selective, peripherally restricted Nav1.7 sodium channel blocker on pain due to diabetic peripheral neuropathy was investigated.