| 中文名称: | 伐地考昔 | ||||
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| 英文名称: | Valdecoxib | ||||
| 别名: | 伐地考昔;戊地昔布 SC 65872 | ||||
| CAS No: | 181695-72-7 | 分子式: | C16H14N2O3S | 分子量: | 314.36 |
| CAS No: | 181695-72-7 | ||||
| 分子式: | C16H14N2O3S | ||||
| 分子量: | 314.36 | ||||
| MDL: | MFCD00950568 | EINEC: | 7302 | ||
| EINEC: | 7302 | ||||
基本信息
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产品编号： |
V10137 |
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产品名称： |
Valdecoxib |
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CAS: |
181695-72-7 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
314.36 |
-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 |
63mg/mL (200.4mM) |
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Ethanol |
18mg/mL (57.25mM) |
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Water |
Insoluble |
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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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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.1811mL |
15.9053mL |
31.8107mL |
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5mM |
0.6362mL |
3.1811mL |
6.3621mL |
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10mM |
0.3181mL |
1.5905mL |
3.1811mL |
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50mM |
0.0636mL |
0.3181mL |
0.6362mL |
生物活性
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产品描述 |
一种高效的，可口服的，选择性的COX-2抑制剂。 |
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靶点 |
COX-2 5nM (IC50) |
COX-1 140μM (IC50) |
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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. |
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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. |
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推荐实验方法(仅供参考)
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激酶实验： |
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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。 |
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细胞实验: |
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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. |
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动物实验: |
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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. |
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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 )
