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Key Documents

PZ0245

Sigma-Aldrich

PF-05105679

≥98% (HPLC)

Synonym(s):

3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid, PF05105679, [(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid

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About This Item

Empirical Formula (Hill Notation):
C26H21FN2O3
CAS Number:
1398583-31-7
Molecular Weight:
428.45
UNSPSC Code:
41116158
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

room temp

Biochem/physiol Actions

PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
PF-05105679 is an antagonist of the TRP (transient receptor potential) channel, also known as the cold and menthol receptor 1 (CMR1), with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling pain, and pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonist, PF-05105679 [(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid] acts as a clinical tool to assess the function of TRPM8 in modulating the body temperature. It also helps to determine its role in the treatment of pain in humans.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
104M4731V

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Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.
Andrews MD, et al.
ACS Medicinal Chemistry Letters, 6(4), 419-424 (2015)

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