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包装规格：1g 5g 25g in glass bottle
溶解性：溶于DMSO（≥34mg/mL）
产品描述：基本信息 产品编号： V10137 产品名称： Valdecoxib CAS: 181695-72-7   储存条件 粉末 2-8℃ 四年     分子式： C16H14N2O3S 溶于液体 -80℃ 6个月 分子量： 314.36 -20℃ 1个月 化学名：  4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide Solubility (25°C)：   体外:   DMSO 63mg/mL (200.4mM) Ethanol 18mg/mL (57.25mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 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。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.1811mL 15.9053mL 31.8107mL 5mM 0.6362mL 3.1811mL 6.3621mL 10mM 0.3181mL 1.5905mL 3.1811mL 50mM 0.0636mL 0.3181mL 0.6362mL   生物活性 产品描述 一种高效的，可口服的，选择性的COX-2抑制剂。 靶点 COX-2 5nM (IC50) COX-1 140μM (IC50)   体外研究 Valdecoxib (Compound 2) is a highly potent,selective and orally active inhibitor of COX-2,with IC50s of 5nM and 140μM for COX-2 and COX-1,respeceively.Valdecoxib (10,100µM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner.Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions. 体内研究 Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema;ED50=10.2±1.4mg/kg).Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model,with an ED50 of 0.032±0.002mg/kg/day.Valdecoxib (10mg/kg,i.p.) significantly attenuates the behavioral and biochemical A(oxidative damage) alterations in chronic-stressed mice.   推荐实验方法(仅供参考) 激酶实验： 体外COX酶测定 COX蛋白在昆虫细胞中的表达，通过评估在COX-1或COX-2杆状病毒培育3天的细胞匀浆中PG合成能力来测定。细胞表达COX-1或COX-2是均质化的，并用花生四烯酸(10μM)培育。COX活性通过监测PG的产生来确定。在模拟感染的Sf9细胞中，没有检测到COX活性。在加入花生四烯酸之前，Valdecoxib用粗1% CHAPS匀浆(2-10微克蛋白质)预培养10分钟。PGE2的形成在培育10分钟后，通过ELISA检测。   细胞实验:   HMEC-1 cells proliferation is measured using the MTT conversion method. Cells are seeded (50.000 cells/well) into 96-well plates. The cells are incubated for 24h with LPS 100µg/mL,CoCl2 200µM,Valdecoxib 10 or 100µM,LPS and Valdecoxib or CoCl2 and Valdecoxib or without tested chemicals (control group). All the substances are added at the same time. After incubation,50µL MTT (1mg/mL) is added and the plates are incubated at 37℃ for 4h.At the end of the experiment,cells are exposed to 100µL DMSO,which enables the release of the blue reaction product-formazan.The absorbance at 570nm is read on a microplate reader and results are expressed as a percentage of the absorbance measured in control cells.   动物实验:   Mice The drugs including naproxen (14mg/kg,i.p.),rofecoxib (5mg/kg,i.p.),meloxicam (5mg/kg,i.p.),nimesulide (5mg/kg,i.p.) and Valdecoxib (10mg/kg,i.p.) are used in the assay.The animals are randomized into 7 groups (n=10 in each group),including the naive group,in which the mice only receive vehicle for 15 d without forced swimming session;the control (chronically stressed) group,in which mice receive vehicle 30 min before the forced swimming session (6 min) for 15 d;the naproxen (14mg/kg) group;the Valdecoxib (10mg/kg) group;the rofecoxib (5mg/kg) group;the meloxicam (5mg/kg) group;and the nimesulide (5mg/kg) group.Drugs are suspended in 0.25% carboxymethylcellulose (CMC) and administered intraperitoneally,30 min before the forced swimming session for 15 consecutive days.
保存条件：2-8℃

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