PF 05105679

Key Product Details

Product Description

PF 05105679 is a selective TRPM8 blocker (IC₅₀ = 103 nM) that exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. PF 05105679 reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. This compound is orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

External Portal Information

The Chemical Probes pages of the Structural Genomics Consortium website are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 05105679 is reviewed.

Product Specifications for PF 05105679

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PF 05105679

The following data is based on the product molecular weight 428.45.

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	2.33 mL	11.67 mL	23.34 mL
5 mM	0.47 mL	2.33 mL	4.67 mL
10 mM	0.23 mL	1.17 mL	2.33 mL
50 mM	0.05 mL	0.23 mL	0.47 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Winchester Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J.Pharmacol.Exp.Ther. 2014 PMID: 25125580
• Andrews Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain. ACS Med.Chem.Lett. 2015 PMID: 25893043

Product Documents for PF 05105679