PF-05105679_product_DataBase

Bioactivity

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].

Invitro

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]. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily[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:

Name

PF-05105679

CAS

1398583-31-7

Formula

C26H21FN2O3

Molar Mass

428.45

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

PF-05105679

CAS: 1398583-31-7 F: C26H21FN2O3 W: 428.45