Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tilmacoxib is a highly selective, time-dependent, and irreversible inhibitor of human COX-2 ( IC50: 85 nM in an enzyme assay).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | Tilmacoxib is a highly selective, time-dependent, and irreversible inhibitor of human COX-2 ( IC50: 85 nM in an enzyme assay). |
靶点活性 | COX-2(human):85 nM |
体外活性 | Tilmacoxib is less potent at inhibiting calcium ionophore-induced thromboxane B2 production in washed human platelets (COX-1) (IC50=6.21 μM). Tilmacoxib inhibits yeast-expressed human recombinant COX-2 (IC50: 0.085 μM), in an enzyme assay. Tilmacoxib does not inhibit human COX-1 prepared from human platelets at concentrations up to 100 μM. Tilmacoxib diminishes lipopolysaccharide-induced prostaglandin E2 production in human peripheral blood mononuclear cells (COX-2) (IC50=15.1 nM), in a cell-based assay. Tilmacoxib displays highly selective inhibition of human COX-2, and its activity is more selective than that of other COX-2 inhibitors (NS-398 and SC-58635). Human recombinant COX-2 activity is attenuated by Tilmacoxib in a dose-dependent and time-dependent manner[1]. Inhibition of proliferation of gastric epithelial cells by a cyclooxygenase 2 inhibitor, Tilmacoxib (JTE522), is also mediated by a PGE2-independent pathway Combination of Tilmacoxib and Arachidonic acid results in marked retardation of wound healing compared to the control, but Tilmacoxib does not completely suppress the increase in cellular PGE2 content following the addition of arachidonate[2]. |
体内活性 | Administration of Tilmacoxib (10 mg/kg) obviously inhibits ACF formation with a 30% reduction in total ACF/colon (p<0.01). The data on crypt multiplicity display that 10 mg/kg Tilmacoxib significantly decreases the formation of foci containing 1-3 crypts but not foci containing four crypts or more. Administration of the low dose of Tilmacoxib (3 mg/kg) has no inhibitory effects on either the total ACF or crypt multiplicity. From the start of the experiment, a total of 80 male F344 rats are treated with 3 or 10 mg/kg of body weight Tilmacoxib or vehicle by oral gavage five times weekly. One week later, rats receive s.c. injections of saline or 20 mg/kg of body weight DMH once weekly for four successive weeks. At the end of 12 weeks after the start of the experiment, all rats are sacrificed and colons are evaluated for ACF. 10 mg/kg Tilmacoxib significantly suppresses the total ACF/colon. No inhibitory effect is observed in the 3 mg/kg Tilmacoxib treatment group [3]. |
别名 | RWJ57504, JTP19605, 替马考昔, JTE522 |
分子量 | 338.4 |
分子式 | C16H19FN2O3S |
CAS No. | 180200-68-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tilmacoxib 180200-68-4 Immunology/Inflammation Neuroscience COX RWJ57504 JTP19605 替马考昔 JTP-19605 JTP 19605 JTE522 RWJ-57504 RWJ 57504 JTE 522 JTE-522 Inhibitor inhibitor inhibit