货号 | 5388/50 |
别名 | 4-[[[3-Chloro-5-(trifluoromethyl)-2 |
供应商 | Tocris |
生物活性 | Potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). Exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 554.85 |
分子式 | C21H13ClF6N2 |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
参考文献 | Ohmiet al (2014) Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg.Med.Chem.Lett. 24 5364. PMID: 25455182. Okamotoet al (2012) Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int.J.Oncol. 40 1431. PMID: 22267123. |