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.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
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.
View Related Products by Product Action
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
Citations are publications that use Tocris products.
Currently there are no citations for PF 05105679. Do you know of a great paper that uses PF 05105679 from Tocris? Please let us know.
Reviews for PF 05105679
There are currently no reviews for this product. Be the first to review PF 05105679 and earn rewards!
Have you used PF 05105679?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.