Background:

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.