PF 05105679

Cat. No. 6003

PF 05105679 C26H21FN2O3 [1398583-31-7]

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

Biological Activity

Selective TRPM8 blocker (IC50 = 103 nM). Exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. Reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Andrews et al (2015) Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain. ACS Med.Chem.Lett. 6 419. PMID: 25893043 .

Winchester et al (2014) Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J.Pharmacol.Exp.Ther. 351 259. PMID: 25125580.

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Keywords: PF 05105679, supplier, PF05105679, selective, transient-receptor-potential, TRPM8, ion, channels, blocks, blockers, orally, bioavailable, Tocris Bioscience, TRPM Blocker products

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