For research use only. Not for therapeutic Use.
PF-05105679 is a selective TRPM8 Antagonist (IC50 = 103 nM) with clinical efficacy in cold-related pain. The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (<28 °C), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia.
| Catalog Number | I008673 |
| CAS Number | 1398583-31-7 |
| Synonyms | PF-05105679; PF 05105679; PF05105679; PF-5105679; PF 5105679; PF5105679.;(R)-3-((N-(1-(4-fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid |
| Molecular Formula | C26H21FN2O3 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IC50 | 103 nM |
| IUPAC Name | 3-[[[(1R)-1-(4-fluorophenyl)ethyl]-(quinoline-3-carbonyl)amino]methyl]benzoic acid |
| InChI | InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1 |
| InChIKey | BXNMZRPTQFVRFA-QGZVFWFLSA-N |
| SMILES | CC(C1=CC=C(C=C1)F)N(CC2=CC=CC(=C2)C(=O)O)C(=O)C3=CC4=CC=CC=C4N=C3 |
| Reference | </br>1: Andrews MD, Af Forselles K, Beaumont K, Galan SR, Glossop PA, Grenie M, Jessiman A, Kenyon AS, Lunn G, Maw G, Owen RM, Pryde DC, Roberts D, Tran TD. Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. ACS Med Chem Lett. 2015 Jan 30;6(4):419-24. doi: 10.1021/ml500479v. eCollection 2015 Apr 9. PubMed PMID: 25893043; PubMed Central PMCID: PMC4394344.</br>2:Winchester WJ, Gore K, Glatt S, Petit W, Gardiner JC, Conlon K, Postlethwaite M, Saintot PP, Roberts S, Gosset JR, Matsuura T, Andrews MD, Glossop PA, Palmer MJ, Clear N, Collins S, Beaumont K, Reynolds DS. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J Pharmacol Exp Ther. 2014 Nov;351(2):259-69. doi: 10.1124/jpet.114.216010. Epub 2014 Aug 14. PubMed PMID: 25125580. |
