Rofecoxib (Synonyms: MK-966) |
Catalog No.GC10516 |
Rofecoxib es un inhibidor de la COX-2 potente, especÍfico y activo por vÍa oral, con IC50 de 26 y 18 nM para la COX-2 humana en células de osteosarcoma humano y células de ovario de hÁmster chino, con una selectividad 1000 veces mayor para la COX-2 que para la COX-2 humana. 1 (IC50 > 50 μM en células U937 y > 15 μM en células de ovario de hÁmster chino).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 162011-90-7
Sample solution is provided at 25 µL, 10mM.
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.
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