1398583-31-7

1398583-31-7 structure

Name: PF 05105679
Chemical Name: 3-({[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino}methyl)benzoic acid
CAS Number: 1398583-31-7
Molecular Formula: C₂₆H₂₁FN₂O₃
Molecular Weight: 428.455
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2018-06-26 05:39:13
Modify Date: 2024-01-16 06:44:39
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].

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

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.

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