PF 05105679

Names

[ 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

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.