PF 05105679

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Cat.No. 6003 - PF 05105679 | C26H21FN2O3 | CAS No. 1398583-31-7
Description: Selective TRPM8 blocker
Chemical Name: 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
Purity: ≥98% (HPLC)

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
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1398583-31-7
PubChem ID 60195662
Smiles C[C@H](C1=CC=C(C=C1)F)N(C(C2=CC3=C(N=C2)C=CC=C3)=O)CC4=CC(C(O)=O)=CC=C4

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 42.84 100
ethanol 42.84 100

Preparing Stock Solutions

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

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

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Product Datasheets

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: 5893043

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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Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Pathways for PF 05105679


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