PF 05089771
Chemical Name: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
Purity: ≥98%
Biological Activity
PF 05089771 is a potent 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.
Cao et al.
Sci.Transl.Med., 2016;8:335ra56 -
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 -
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.
J.Med.Chem., 2017;60:7029
Product Datasheets
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Citations for PF 05089771
The citations listed below are publications that use Tocris products. Selected citations for PF 05089771 include:
6 Citations: Showing 1 - 6
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Ectopic expression of Nav1.7 in spinal dorsal horn neurons induced by NGF contributes to neuropathic pain in a mouse spinal cord injury model.
Authors: Wei Et al.
Front Mol Neurosci 2023;16:1091096
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Bringing to light the physiological and pathological firing patterns of human induced pluripotent stem cell-derived neurons using optical recordings.
Authors: Oliver Et al.
Front Cell Neurosci 2023;16:1039957
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NaV1.1 is essential for proprioceptive signaling and motor behaviors.
Authors: Darik A Et al.
Elife 2022;11
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A central mechanism of analgesia in mice and humans lacking the sodium channel NaV1.7.
Authors: Jing Et al.
Neuron 2021;109:1497-1512.e6
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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.
Theranostics 2019;9:4287
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Tetrodotoxin-Sensitive Sodium Channels Mediate Action Potential Firing and Excitability in Menthol-Sensitive Vglut3-Lineage Sensory Neurons.
Authors: Ellen A Et al.
J Neurosci 2019;39:7086-7101
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