| 中文名称: | 替马考昔 | ||||
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| 英文名称: | Tilmacoxib | ||||
| 别名: | JTE522; JTP19605; RWJ57504 | ||||
| CAS No: | 180200-68-4 | 分子式: | C16H19FN2O3S | 分子量: | 338.4 |
| CAS No: | 180200-68-4 | ||||
| 分子式: | C16H19FN2O3S | ||||
| 分子量: | 338.4 | ||||
基本信息
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产品编号： |
T11004 |
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产品名称： |
Tilmacoxib |
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CAS: |
180200-68-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
338.40 |
-20℃ |
1个月 |
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化学名： |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种高度选择性的,时间依赖性的，及不可逆的COX-2抑制剂。 |
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靶点 |
Human COX-2 85nM (IC50) |
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体外研究 |
Inhibitory activity and the mechanism of action of Tilmacoxib (JTE-522),a novel selective cyclooxygenase (COX)-2 inhibitor,on human COX-1 and COX-2 are investigated and compared with those of reference compounds.In an enzyme assay,Tilmacoxib inhibits yeast-expressed human recombinant COX-2 with an IC50 of 0.085μM. In contrast,Tilmacoxib does not inhibit human COX-1 prepared from human platelets at concentrations up to 100μM.In a cell-based assay,Tilmacoxib diminishes lipopolysaccharide-induced prostaglandin E2 production in human peripheral blood mononuclear cells (COX-2) (IC50=15.1nM).On the other hand,Tilmacoxib is less potent at inhibiting calcium ionophore-induced thromboxane B2 production in washed human platelets (COX-1) (IC50=6.21μM).Tilmacoxib shows 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.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 a 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. |
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体内研究 |
The present experiment is designed to assess the potential chemopreventive properties of Tilmacoxib (JTE-522),a new selective cyclooxygenase-2 inhibitor,on the induction of 1,2-dimethylhydrazine (DMH)-induced colonic aberrant crypt foci (ACF),a marker of rat colon carcinogenesis.A total of 80 male F344 rats are treated with 3 or 10mg/kg of body weight Tilmacoxib or vehicle by oral gavage five times weekly from the start of the experiment.One week later,rats receive s.c.injections of saline or 20mg/kg of body weight DMH once weekly for four successive weeks.At the end of 12 weeks after the start of experiment,all rats are sacrificed and colons are evaluated for ACF.10mg/kg Tilmacoxib significantly suppresses the total ACF/colon. No inhibitory effect is observed in the 3mg/kg Tilmacoxib treatment group.Administration of 10mg/kg Tilmacoxib significantly suppresses ACF formation with a 30% reduction in total ACF/colon (p<0.01).Furthermore,the data on crypt multiplicity show that 10mg/kg Tilmacoxib significantly reduces the formation of foci containing 1-3 crypts but not foci containing four crypts or more.Administration of the low dose of Tilmacoxib (3mg/kg) has no inhibitory effects on either the total ACF or crypt multiplicity. |
推荐实验方法(仅供参考)
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细胞实验: |
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Tilmacoxib is resolved with DMSO prior to the experiment and concentrations of 1-100μM are assessed.Effects of Arachidonic acid are assessed at concentrations of 0,5 and 20μg/mL.Further,the combination of Tilmacoxib (100μM) with Arachidonic acid (20μg/mL) is assessed in additional experiments.Circular artificial wounds are created after formation of complete monolayer cell sheets.Tilmacoxib and Arachidonic acid are added just after wound formation.The process of epithelial restoration is monitored by measuring the cell-free area using an inverted phase-contrast microscope every 24h.Changes in the cell-free area during restoration are analyzed quantitatively with an image analyser. |
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动物实验: |
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Rats A total of 80 male F344 rats,5 weeks old,are used.Rats at 6 weeks of age after 1 week of acclimatization are divided randomly into five groups.The rats in groups 1-3 (20 rats each) are injected s.c.with DMH (20mg/kg body wt) from 1 week after the start of the experiment,once weekly for four successive weeks.Those in groups 4 and 5 (10 rats each) are injected s.c.with 0.9% saline at the same time.Group 2 is treated with Tilmacoxib at a dose of 3mg/kg body wt by oral gavage,five times weekly from the start of the experiment to the end of the experiment. Groups 3 and 5 are treated with Tilmacoxib at the dose of 10mg/kg body wt in the same manner as group 2.Groups 1 and 4 are treated with 0.5% CMC alone,without Tilmacoxib.Body weight,water and food consumption are measured weekly during the experiment. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
