PF-05105679 是一种具有口服活性的选择性 TRPM8 拮抗剂，IC50 为 103 nM。
货号:ajcx20720
CAS:1398583-31-7
分子式:C26H21FN2O3
分子量：428.5
溶解度:DMSO: 10 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-05105679 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 = 103 nM for inhibition of voltage-activated currents in HEK293 cells expressing the human receptor).1 It is greater than 100-fold selective for TRPM8 over a panel of 90 receptors, ion channels, and enzymes. PF-05105679 inhibits calcium flux induced by cold or the TRPM8 agonist WS-12 in HEK293 cells expressing the human TRPM8 (IC50s = 480 and 181 nM, respectively). Intravenous infusion of PF-05105679 (46.67 μg/kg per minute) reverses cold-induced reductions in bladder capacity in anesthetized guinea pigs. It decreases the core body temperature in rats when administered at doses of 100 and 300 mg/kg.

|1. Winchester, W.J., Gore, K., Glatt, S., et al. Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J. Pharmacol. Exp. Ther. 351(2), 259-269 (2014).