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Submit ReviewPF 05105679
Discontinued Product
PF 05105679 (Cat. No. 6003) has been withdrawn from sale for commercial reasons.
Description: Selective TRPM8 blocker
Chemical Name: 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
Purity: ≥98% (HPLC)
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 |
| InChI Key | BXNMZRPTQFVRFA-QGZVFWFLSA-N |
| 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.
Product Datasheets for PF 05105679
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
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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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Currently there are no citations for PF 05105679.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Pain Research Product Guide
A collection of over 280 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.