WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522489
Description: 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.
MedKoo Cat#: 522489
Chemical Formula: C26H21FN2O3
Exact Mass: 428.15362
Molecular Weight: 428.4634
Elemental Analysis: C, 72.89; H, 4.94; F, 4.43; N, 6.54; O, 11.20
Synonym: PF-05105679; PF 05105679; PF05105679; PF-5105679; PF 5105679; PF5105679.
IUPAC/Chemical Name: (R)-3-((N-(1-(4-fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid
InChi Key: BXNMZRPTQFVRFA-QGZVFWFLSA-N
InChi Code: 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
SMILES Code: O=C(O)C1=CC=CC(CN([C@@H](C2=CC=C(F)C=C2)C)C(C3=CC4=CC=CC=C4N=C3)=O)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 428.4634 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||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.
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: