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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Rofecoxib (formerly MK-0966; MK0966; MK-966; MK966; Vioxx; Ceoxx; Ceeoxx.), an NSAID drug, is a potent and selective COX-2 inhibitor with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 of 18 NM. Rofecoxib belongs to the nonsteroidal anti-inflammatory drug (NSAID) class and has now been withdrawn from the market due to safety concerns. Rofecoxib exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of rofecoxib is believed to be due to inhibition of prostaglandin synthesis, via inhibition of cyclooxygenase-2 (COX-2).
| ln Vitro |
In human osteosarcoma cells and Chinese hamster ovary cells, rofecoxib (MK-0966) has IC50s of 26 and 18 nM for human COX-2, respectively. It has 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 is a strong and oral active inhibitor of COX-2. Rofecoxib suppresses purified human COX-1 in a non-time-dependent way that is only visible at extremely low substrate concentrations (IC50=26 μM at 0.1 μM arachidonic acid concentration), whereas it time-dependently inhibits purified human recombinant COX-2 (IC50=0.34 μM). When it comes to the suppression of COX-1-derived thromboxane B(2) synthesis after blood coagulation, rofecoxib has a higher IC50 value of 18.8 ± 0.9 μM than lipopolysaccharide-induced, COX-2-derived PGE(2) synthesis [1]. Cell proliferation is induced by ropecoxib (36 μM) at 68% in MPP89, 58% in Ist-Mes-1, and 40% in Ist-Mes-2. The survival rates of MSTO-211H and NCI-H2452 after receiving 36 μM of rofecoxib are 97% and 90%, respectively. In Ist-Mes-1, Ist-Mes-2, and MPP89 cell lines, ropecoxib (36 μM) reduces the levels of COX-2 and mRNA[3].
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| ln Vivo |
In mouse models, rofecoxib potently suppresses the following: lipopolysaccharide-induced pyresis (ID50=0.24 mg/kg), carrageenan-induced paw edema (ID50=1.5 mg/kg), and adjuvant-induced arthritis (ID50=0.74 mg/kg/day). In rats, rofecoxib also prevents the degradation of bone and cartilage caused by adjuvants. Ropecoxib has no effect at doses up to 200 mg/kg/day for five days in a 51Cr excretion experiment used to assess gastrointestinal integrity in either rats or squirrel monkeys[1]. In mice, the blood vessels connected to the internal limiting membrane (ILM) are diminished by rofecoxib (15 mg/kg, ip). In ROP mice, Rofecoxib also greatly reduces the expressions of the COX-2 and VEGF proteins, as well as the COX-2 and VEGF mRNAs[2].
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| References |
[1]. 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.
[2]. 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. [3]. Stoppoloni D, et al. Synergistic effect of gefitinib and rofecoxib in mesothelioma cells. Mol Cancer. 2010 Feb 2;9:27 |
| Molecular Formula |
C17H14O4S
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| Molecular Weight |
314.36
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| CAS # |
162011-90-7
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| Related CAS # |
Rofecoxib-d5;544684-93-7
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| SMILES |
S(C([H])([H])[H])(C1C([H])=C([H])C(=C([H])C=1[H])C1C([H])([H])OC(C=1C1C([H])=C([H])C([H])=C([H])C=1[H])=O)(=O)=O
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| Synonyms |
MK-0966; MK0966; MK0966; MK966; MK966; MK 966; MK 0966; Trade name: Vioxx; Ceoxx; Ceeoxx.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1811 mL | 15.9053 mL | 31.8107 mL | |
| 5 mM | 0.6362 mL | 3.1811 mL | 6.3621 mL | |
| 10 mM | 0.3181 mL | 1.5905 mL | 3.1811 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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