A COX-2 inhibitor
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].
参考文献:
[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.
| Cell experiment [1]: | |
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Cell lines |
Osteosarcoma cells and U937 cells |
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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. |
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Reacting condition |
15 mins |
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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]: | |
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Animal models |
Rat adjuvant-induced arthritis model |
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Dosage form |
0.1, 0.3, 1.0 and 3.0 mg/kg/day; p.o. |
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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. |
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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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参考文献: [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. |
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