PF 05089771

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Cat.No. 5931 - PF 05089771 | C18H12Cl2FN5O3S2.C7H8O3S | CAS No. 1430806-04-4
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 67.26 100

Preparing Stock Solutions

The following data is based on the product molecular weight 672.56. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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


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