Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC₅₀s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC₅₀ > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).

Rofecoxib (MK-0966) is a potent and orally active inhibitor of COX-2, with IC₅₀s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over COX-1 (IC₅₀ >50 μM in U937 cells and >15 μM in Chinese hamster ovary cells). Rofecoxib time dependently inhibits purified human recombinant COX-2 (IC₅₀=0.34 μM) but suppresses purified human COX-1 in a non-time-dependent manner that can only be observed at a very low substrate concentration (IC₅₀=26 μM at 0.1 μM arachidonic acid concentration). Rofecoxib selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE(2) synthesis with an IC₅₀ value of 0.53 ± 0.02 μM compared with an IC₅₀ value of 18.8 ± 0.9 μM for the inhibition of COX-1-derived thromboxane B(2) synthesis after blood coagulation. Rofecoxib (36 μM) causes a cell proliferation of 68% in MPP89, of 58% in Ist-Mes-1 and 40% in Ist-Mes-2. MSTO-211H and NCI-H2452 treated with 36 μM of Rofecoxib have a survival of 97% and 90% respectively. Rofecoxib (36 μM) decreases COX-2 and mRNA levels in Ist-Mes-1, Ist-Mes-2 and MPP89 cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Rofecoxib potently inhibits carrageenan-induced paw edema (ID₅₀=1.5 mg/kg), carrageenan-induced paw hyperalgesia (ID₅₀=1.0 mg/kg), lipopolysaccharide-induced pyresis (ID₅₀=0.24 mg/kg), and adjuvant-induced arthritis (ID₅₀=0.74 mg/kg/day) in rodent models. Rofecoxib also protects adjuvant-induced destruction of cartilage and bone structures in rats. In a ⁵¹Cr excretion assay for detection of gastrointestinal integrity in either rats or squirrel monkeys, rofecoxib shows no effect at doses up to 200 mg/kg/day for 5 days. Rofecoxib (15 mg/kg, i.p.) reduces the blood vessels attached to the internal limiting membrane (ILM) in mice. COX-2 and VEGF protein expressions, COX-2 mRNA and VEGF mRNA are also significantly decreased by Rofecoxib in ROP mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Rofecoxib potently inhibits carrageenan-induced paw edema (ID₅₀=1.5 mg/kg), carrageenan-induced paw hyperalgesia (ID₅₀=1.0 mg/kg), lipopolysaccharide-induced pyresis (ID₅₀=0.24 mg/kg), and adjuvant-induced arthritis (ID₅₀=0.74 mg/kg/day) in rodent models. Rofecoxib also protects adjuvant-induced destruction of cartilage and bone structures in rats. In a ⁵¹Cr excretion assay for detection of gastrointestinal integrity in either rats or squirrel monkeys, rofecoxib shows no effect at doses up to 200 mg/kg/day for 5 days. Rofecoxib (15 mg/kg, i.p.) reduces the blood vessels attached to the internal limiting membrane (ILM) in mice. COX-2 and VEGF protein expressions, COX-2 mRNA and VEGF mRNA are also significantly decreased by Rofecoxib in ROP mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Rofecoxib, 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. J Pharmacol Exp Ther. 1999 Aug;290(2):551-60.  [Content Brief]

  . Liu NN, et al. Rofecoxib inhibits retinal neovascularization via down regulation of cyclooxygenase-2 and vascular endothelial growth factor expression. Clin Exp Ophthalmol. 2015 Jul;43(5):458-65.  [Content Brief]

  . Stoppoloni D, et al. Synergistic effect of gefitinib and rofecoxib in mesothelioma cells. Mol Cancer. 2010 Feb 2;9:27.  [Content Brief]