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PF 05105679

Catalog #: 6003 Datasheet / COA / SDS

Discontinued Product

6003 has been discontinued.
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PF 05105679 | CAS No. 1398583-31-7 | TRPM Blockers
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Description: Selective TRPM8 blocker

Chemical Name: 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid

Purity: ≥98%

Product Details
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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.

Technical Data

M.Wt:
428.45
Formula:
C26H21FN2O3
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at RT
CAS No:
1398583-31-7

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc

Background References

  1. Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain.
    Andrews et al.
    ACS Med.Chem.Lett., 2015;6:419
  2. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans.
    Winchester et al.
    J.Pharmacol.Exp.Ther., 2014;351:259

Product Datasheets

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