PF 05105679

Modify Date: 2024-01-16 06:44:39

PF 05105679 Structure
PF 05105679 structure
Common Name PF 05105679
CAS Number 1398583-31-7 Molecular Weight 428.455
Density 1.3±0.1 g/cm3 Boiling Point 669.0±55.0 °C at 760 mmHg
Molecular Formula C26H21FN2O3 Melting Point N/A
MSDS Chinese USA Flash Point 358.4±31.5 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of PF 05105679


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].

 Names

Name 3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid
Synonym More Synonyms

 PF 05105679 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
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
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport

 Synonyms

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