GlpBio

Rofecoxib

目录号: GC10516纯度: >99.50%同义词: 罗非考昔; MK 966
A COX-2 inhibitor
Rofecoxib
Cas No.: 162011-90-7
规格价格库存数量操作
100mg¥410.00现货
1
250mg¥893.00现货
1
10mM (in 1mL DMSO)¥441.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

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产品描述 Description

Rofecoxib is a potent and orally active inhibitor of cyclooxygenase (COX)-2 with IC50 value of 0.34μM [1].

Rofecoxib is an inhibitor of COX-2 and is developed as a new class of anti-inflammatory agents with improved gastrointestinal tolerability. It has been shown to be effective in the treatment of osteoarthritis. Rofecoxib potently inhibits COX-2 in cell-based assays with IC50 values ranging from 18nM to 46nM. In osteosarcoma cells, rofecoxib prevents the production of PGE2 with IC50 value of 26nM. Rofecoxib also shows effective inhibition of recombinant human COX-2 in stably transfected CHO cells with IC50 value of 18nM. Besides that, rofecoxib inhibits the activity of purified human COX-2 with IC50 value of 0.34μM in the in vitro assay with Genapol X-100 [1].

In the carrageenan-induced rat paw edema assay, administration of rofecoxib suppresses the edema response with ID50 value of 1.5mg/kg. And in rats with carrageenan-induced paw hyperalgesia, relieves the hyperalgesia with ID50 value of 1mg/kg [1].

References:
[1] Chan C C, Boyce S, Brideau C, et al. Rofecoxib [Vioxx, MK-0966; 4-(4′-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. Journal of Pharmacology and Experimental Therapeutics, 1999, 290(2): 551-560.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Osteosarcoma cells and U937 cells

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

15 mins

Applications

In osteosarcoma cells (COX-2), Rofecoxib inhibited the arachidonic acid-dependent production of PGE2 by with an IC50 value of 26 ± 10 nM. However, in U937 cells (COX-1), Rofecoxib inhibited the arachidonic acid-dependent production of PGE2 with an IC50 value over 50 mM. It was indicated that Rofecoxib was a potent and selective inhibitor of human COX-2 in cell-based assays.
Animal experiment [1]:

Animal models

Rat adjuvant-induced arthritis model

Dosage form

0.1, 0.3, 1.0 and 3.0 mg/kg/day; p.o.

Applications

Rofecoxib significantly inhibited carrageenan-induced paw edema and paw hyperalgesia, as well as lipopolysaccharide-induced pyresis with the IC50 values of 1.5 mg/kg, 1.0 mg/kg and 0.24 mg/kg, respectively. Besides, Rofecoxib also blocked adjuvant-induced arthritis with an IC50 value of 0.74 mg/day. In addition, Rofecoxib also showed a protective effect on adjuvant-induced destruction of cartilage and bone structures.

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]. Chan C C, Boyce S, Brideau C, et al. Rofecoxib [Vioxx, MK-0966; 4-(4′-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. Journal of Pharmacology and Experimental Therapeutics, 1999, 290(2): 551-560.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
162011-90-7
同义词
罗非考昔; MK 966
化学名
3-(4-methylsulfonylphenyl)-4-phenyl-2H-furan-5-one
SMILES
CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3
分子式
C17H14O4S
分子量
314.36 g/mol
溶解性
≥ 15.72mg/mL in DMSO
保存条件
Store at 2-8°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