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PF 05105679

Names

[ CAS No. ]:
1398583-31-7

[ Name ]:
PF 05105679

[Synonym ]:
Benzoic acid, 3-[[[(1R)-1-(4-fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-
3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid

Biological Activity

[Description]:

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily. PF-05105679 is used for clinical efficacy in cold-related pain[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Neurological Disease

[Target]

TRPM8:103 nM (IC50)


[In Vitro]

PF-05105679 demonstrates >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels[1].

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
669.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H21FN2O3

[ Molecular Weight ]:
428.455

[ Flash Point ]:
358.4±31.5 °C

[ Exact Mass ]:
428.153625

[ LogP ]:
4.57

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.661

[ Storage condition ]:
-20°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Related Compounds