Rofecoxib (Synonyms: MK-966)

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 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.