替马考昔,Tilmacoxib

替马考昔|T15630|TargetMol

价格 17500 10600 13800
包装 100mg 25mg 50mg
最小起订量 25mg
发货地 上海
更新日期 2026-04-02
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产品详情

中文名称:替马考昔英文名称:Tilmacoxib
CAS:180200-68-4品牌: TargetMol
产地: 美国保存条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
产品类别: 抑制剂
货号: T15630
2026-04-02 替马考昔 Tilmacoxib 100mg/17500RMB;25mg/10600RMB;50mg/13800RMB 17500 TargetMol 美国 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 抑制剂

Product Introduction

Bioactivity

名称Tilmacoxib
描述Tilmacoxib is a highly selective, time-dependent, and irreversible inhibitor of human COX-2 ( IC50: 85 nM in an enzyme assay).
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].
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
关键字Tilmacoxib | RWJ-57504 | RWJ 57504 | JTP-19605 | JTP 19605 | JTE-522 | JTE 522 | Human COX-2
相关产品Trometamol | Gallic Acid Monohydrate | Naproxen sodium | 4-Aminosalicylic acid | 5-Methylfurfural | Phenylbutazone | Indomethacin | Paradol | Acetaminophen | Diclofenac Potassium | Magnesium sulfate | Phenidone
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关键字: 替马考昔|||RWJ57504|||JTP19605|||JTE522|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。
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