PF 05089771
Tocris Bioscience | Catalog # 5931
Key Product Details
Description
Product Description
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.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Product Specifications for PF 05089771
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 67.26 | 100 |
Preparing Stock Solutions for PF 05089771
The following data is based on the product molecular weight 672.56.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.49 mL | 7.43 mL | 14.87 mL |
| 5 mM | 0.30 mL | 1.49 mL | 2.97 mL |
| 10 mM | 0.15 mL | 0.74 mL | 1.49 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.30 mL |
Calculators
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 25 publications citing the usage of this product.
- Alexandrou Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release. PLoS One 2016 PMID: 27050761
- Swain 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 J.Med.Chem. 2017 PMID: 28682065
- Cao Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci.Transl.Med. 2016 PMID: 27099175
Product Documents for PF 05089771
Product Specific Notices for PF 05089771
For research use only
Related Research Areas
Citations for PF 05089771
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Species: HumanVerified Customer | Posted 12/26/2019The effect of PF-05089771, a selective, peripherally restricted Nav1.7 sodium channel blocker on pain due to diabetic peripheral neuropathy was investigated.
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