Valdecoxib
(Synonyms: 伐地考昔; SC 65872) 目录号 : GC14020
A COX-2 inhibitor
Cas No.:181695-72-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| In vitro experiment [1]: | |
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Samples |
Whole blood |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
Overnight for assessment of the extent of COX-2 inhibition; 25 mins for assessment of the extent of COX-1 inhibition |
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Applications |
In the assay for assessment of the extent of COX-2 inhibition, Valdecoxib inhibited lipopolysaccharide-induced PGE2 production, with an IC50 value of 0.89 μM. In the assay for assessment of the extent of COX-1 inhibition, Valdecoxib inhibited TXB2 production, with an IC50 value of 25.4 μM. |
| Animal experiment [1]: | |
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Animal models |
Male SD rats |
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Dosage form |
0.02, 0.032 or 10.2 mg/kg; p.o. |
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Applications |
In SD rats, Valdecoxib inhibited carrageenan-induced foot pad edema, with an ED50 value of 10.2 mg/kg. In a rat adjuvant arthritis model, Valdecoxib also showed chronic anti-inflammatory activity, with an ED50 value of 0.032 mg/kg/day. In addition, Valdecoxib inhibited prostaglandin production at the inflammatory site in a carrageenan-induced air pouch model, with an ED50 value of 0.02 mg/kg. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Talley J J, Brown D L, Carter J S, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]-benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. Journal of medicinal chemistry, 2000, 43(5): 775-777. | |
Valdecoxib is a potent and selective inhibitor of cyclooxygenase-2 (COX-2) with IC50 value of 5nM [1].
Valdecoxib is developed for the management of pain and inflammation. Valdecoxib and its intravenous prodrug parecoxib exert significant opioid-sparing effects after dental, gynecologic, orthopedic and other noncardiac surgical procedures. In the cellular assay, valdecoxib shows inhibitory activity on human recombinant COX-2 with IC50 value of 5nM. It shows no significant effect on COX-1 with IC50 value of 140μM. In the ex vivo assay using human whole blood, valdecoxib prevents PGE2 production with IC50 value of 0.89μM. Moreover, oral administration of valdecoxib exerts chronic anti-inflammatory activity with ED50 value of 0.032 mg/kg/day in the rat adjuvant arthritis model. In addition, valdecoxib is reported to have cardiovascular risk adverse effect in patients undergoing CABG [1, 2].
References:
[1] Talley J J, Brown D L, Carter J S, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]-benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. Journal of medicinal chemistry, 2000, 43(5): 775-777.
[2] Nussmeier N A, Whelton A A, Brown M T, et al. Complications of the COX-2 inhibitors parecoxib and valdecoxib after cardiac surgery. New England Journal of Medicine, 2005, 352(11): 1081-1091.
| Cas No. | 181695-72-7 | SDF | |
| 别名 | 伐地考昔; SC 65872 | ||
| 化学名 | 4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide | ||
| Canonical SMILES | CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N | ||
| 分子式 | C16H14N2O3S | 分子量 | 314.36 |
| 溶解度 | ≥ 15.72mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1811 mL | 15.9053 mL | 31.8107 mL |
| 5 mM | 0.6362 mL | 3.1811 mL | 6.3621 mL |
| 10 mM | 0.3181 mL | 1.5905 mL | 3.1811 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。