PF-05105679

产品说明书

Print
Chemical Structure| 1398583-31-7 同义名 : -
CAS号 : 1398583-31-7
货号 : A104047
分子式 : C26H21FN2O3
纯度 : 99%+
分子量 : 428.45
MDL号 : MFCD28386022
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 PF-05105679 is an orally-bioavailable and selective TRPM8 blocker (IC50 = 103 nM) which exhibits > 100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.67mL

2.33mL

1.17mL

23.34mL

4.67mL

2.33mL
参考文献

[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.

[2]Winchester WJ, Gore K, et al. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J Pharmacol Exp Ther. 2014 Nov;351(2):259-69.