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)
Literature (2)

Biological Activity for PF 05105679

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 for PF 05105679

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 for PF 05105679

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 05105679

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

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 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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References for PF 05105679

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

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

If you know of a relevant reference for PF 05105679, please let us know.

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Keywords: PF 05105679, PF 05105679 supplier, PF05105679, selective, transient-receptor-potential, TRPM8, ion, channels, blocks, blockers, orally, bioavailable, TRPM, 6003, Tocris Bioscience

Citations for PF 05105679

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