Basic information Safety Supplier Related

PF 05105679

Basic information Safety Supplier Related

PF 05105679 Basic information

Product Name:
PF 05105679
Synonyms:
  • PF 05105679
  • 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]benzoic acid
  • Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-
  • PF-05105679 >=98% (HPLC)
  • Inhibitor,TRPM8,PF05105679,subfamily,cold-related,orally,clinical,menthol,TRP Channel,PF-05105679,pain,Transient receptor potential channels,PF 05105679,inhibit,cold,CMR1,melastatin
  • (R)-3-((N-(1-(4-Fluorophenyl)ethyl)quinoline-3-carboxamido)methyl)benzoic acid
  • PF-05105679, 10 mM in DMSO
  • PF 0510567
CAS:
1398583-31-7
MF:
C26H21FN2O3
MW:
428.45
Mol File:
1398583-31-7.mol
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PF 05105679 Chemical Properties

Boiling point:
669.0±55.0 °C(Predicted)
Density 
1.308±0.06 g/cm3(Predicted)
storage temp. 
room temp
solubility 
DMSO: 10 mg/ml
form 
powder
pka
4.14±0.10(Predicted)
color 
white to beige
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PF 05105679 Usage And Synthesis

Uses

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain[1].

Biological Activity

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.

in vivo

PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) has a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs[1].
PF-05105679 (2, 20 mg/kg) has a T1/2 of 3.6 hours, a CL of 19.8 mL/min/kg, and a Vss of 6.2 L/kg for rats[1].

Animal Model:Male beagle dogs (weight 10 to 15kg)[1]
Dosage:0.2 mg/kg (iv) or 20 mg/kg (oral gavage)(Pharmacokinetic Analysis)
Administration:Iv or oral gavage
Result:Had a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs.

IC 50

TRPM8: 103 nM (IC50)

References

[1] Andrews MD, et al. 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

PF 05105679Supplier

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Email
info@chemlin.com.cn
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Email
3008007409@qq.com
Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Email
klq@cw-bio.com
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