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Submit ReviewPF 05089771
Description: Potent and selective Nav1.7 channel blocker
Chemical Name: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
Purity: ≥98% (HPLC)
Biological Activity for PF 05089771
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.
Compound Libraries for PF 05089771
PF 05089771 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 05089771
| M. Wt | 672.56 |
| Formula | C18H12Cl2FN5O3S2.C7H8O3S |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1430806-04-4 |
| PubChem ID | 71554187 |
| InChI Key | NVKBPDYKPNYMDR-UHFFFAOYSA-N |
| Smiles | ClC1=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C(F)C(S(NC4=CSC=N4)(=O)=O)=C1.CC5=CC=C(S(=O)(O)=O)C=C5 |
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.
Solubility Data for PF 05089771
| 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 will 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 | 0.3 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 | 0.3 mL |
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Product Datasheets for PF 05089771
References for PF 05089771
References are publications that support the biological activity of the product.
Cao et al (2016) Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci.Transl.Med. 8 335ra56 PMID: 27099175
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 PMID: 27050761
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 J.Med.Chem. 60 7029 PMID: 28682065
If you know of a relevant reference for PF 05089771, please let us know.
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Keywords: PF 05089771, PF 05089771 supplier, PF05089771, potent, selective, Nav1.7, sodium, channels, neuropathic, pain, Voltage-gated, Sodium, Channels, 5931, Tocris Bioscience
6 Citations for PF 05089771
Citations are publications that use Tocris products. Selected citations for PF 05089771 include:
Oliver et al (2023) Bringing to light the physiological and pathological firing patterns of human induced pluripotent stem cell-derived neurons using optical recordings. Front Cell Neurosci 16 1039957 PMID: 36733665
Wei et al (2023) Ectopic expression of Nav1.7 in spinal dorsal horn neurons induced by NGF contributes to neuropathic pain in a mouse spinal cord injury model. Front Mol Neurosci 16 1091096 PMID: 36937049
Jing et al (2021) A central mechanism of analgesia in mice and humans lacking the sodium channel NaV1.7. Neuron 109 1497-1512.e6 PMID: 33823138
Darik A et al (2022) NaV1.1 is essential for proprioceptive signaling and motor behaviors. Elife 11 PMID: 36278870
Ellen A et al (2019) Tetrodotoxin-Sensitive Sodium Channels Mediate Action Potential Firing and Excitability in Menthol-Sensitive Vglut3-Lineage Sensory Neurons. J Neurosci 39 7086-7101 PMID: 31300524
Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762
Do you know of a great paper that uses PF 05089771 from Tocris? Please let us know.
Reviews for PF 05089771
Average Rating: 5 (Based on 1 Review.)
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Study of PF 05089771's Nav1.7 blocking efficacy.
By
Anonymous on 12/26/2019
Species: Human
The 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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