PF 05089771

Product Description

PF 05089771 is a potent and selective Na_v1.7 channel blocker (IC₅₀ = 8, 11 and 171 nM for mouse, human and rat Na_v1.7, respectively). Exhibits selectivity for Na_v1.7 over other Na_v1 channels (IC₅₀ values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Na_v1.2, Na_v1.6, Na_v1.1, Na_v1.4, Na_v1.3 and Na_v1.5, 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.

Solubility

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.

Select a batch to recalculate based on the batch molecular weight:

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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.

• Alexandrou Subtype-selective small molecule inhibitors reveal a fundamental role for Na_v1.7 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