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
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
Biological target:
PF-05105679 is a selective TRPM8 Antagonist (IC50 = 103 nM) with clinical efficacy in cold-related pain.
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
10.0 |
23.34 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
428.46
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:
25125580.
Gosset JR, Beaumont K, Matsuura T, Winchester W, Attkins N, Glatt S, Lightbown I, Ulrich K, Roberts S, Harris J, Mesic E, van Steeg T, Hijdra D, van der Graaf PH. A cross-species translational pharmacokinetic-pharmacodynamic evaluation of core body temperature reduction by the TRPM8 blocker PF-05105679. Eur J Pharm Sci. 2017 Nov 15;109S:S161-S167. doi: 10.1016/j.ejps.2017.06.009. Epub 2017 Jun 7. PMID: 28603038.
