PF-05105679
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MedKoo CAT#: 522489

CAS#: 1398583-31-7

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.


Chemical Structure

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PF-05105679
CAS# 1398583-31-7

Theoretical Analysis

MedKoo Cat#: 522489
Name: PF-05105679
CAS#: 1398583-31-7
Chemical Formula: C26H21FN2O3
Exact Mass: 428.15
Molecular Weight: 428.463
Elemental Analysis: C, 72.89; H, 4.94; F, 4.43; N, 6.54; O, 11.20

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2250 2 Weeks
1g USD 3250 2 Weeks
2g USD 5850 2 Weeks
Bulk inquiry

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

More Info:

Product Data:
Biological target: PF-05105679 is a selective TRPM8 Antagonist (IC50 = 103 nM) with clinical efficacy in cold-related pain.
In vitro activity: TBD
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.0 23.34

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.

Recalculate based on batch purity %
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
Formulation protocol: TBD
In vitro protocol: TBD
In vivo protocol: TBD

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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.