货号 | 6003/10 |
别名 | 3-[[[(1R)-1-(4-Fluorophenyl)ethyl]( |
供应商 | Tocris |
生物活性 | Selective TRPM8 blocker (IC50 = 103 nM). Exhibits >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. Reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. Orally bioavailable. |
运输条件 | Ambient |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 428.45 |
分子式 | C26H21FN2O3< |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
参考文献 | Andrewset al (2015) Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain. ACS Med.Chem.Lett. 6 419. PMID: 25893043. Winchesteret al (2014) Inhibition of TRPM8 channels reduces pain in the cold pressor test in humans. J.Pharmacol.Exp.Ther. 351 259. PMID: 25125580. |