GlpBio

Valdecoxib

目录号: GC14020纯度: >99.50%同义词: 伐地考昔; SC 65872
A COX-2 inhibitor
Valdecoxib
Cas No.: 181695-72-7
规格价格库存数量操作
10mg¥620.00现货
1
50mg¥2,478.00现货
1
10mM (in 1mL DMSO)¥368.00现货
1
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文献被引

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    183(7):1867-1883 (2020)
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

In vitro experiment [1]:

Samples

Whole blood

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

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]:

Animal models

Male SD rats

Dosage form

0.02, 0.032 or 10.2 mg/kg; p.o.

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.

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.

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
181695-72-7
同义词
伐地考昔; SC 65872
化学名
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide
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 g/mol
溶解性
≥ 15.72mg/mL in DMSO
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol