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PF-05105679
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-05105679图片
CAS NO:1398583-31-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
PF-05105679 是一种具有口服活性的选择性 TRPM8 拮抗剂,IC50 为 103 nM。
Cas No.1398583-31-7
Canonical SMILESO=C(N([C@@H](C1=CC=C(F)C=C1)C)CC2=CC=CC(C(O)=O)=C2)C3=CC4=C(C=CC=C4)N=C3
分子式C26H21FN2O3
分子量428.5
溶解度DMSO: 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).