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.
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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.
| Cell experiment [1]: | |
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Cell lines |
Osteosarcoma cells and U937 cells |
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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 |
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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 experiment [1]: | |
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Animal models |
Rat adjuvant-induced arthritis model |
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Dosage form |
0.1, 0.3, 1.0 and 3.0 mg/kg/day; p.o. |
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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. |
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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. |
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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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| Cas No. | 162011-90-7 | SDF | |
| Sinónimos | MK-966 | ||
| Chemical Name | 3-(4-methylsulfonylphenyl)-4-phenyl-2H-furan-5-one | ||
| Canonical SMILES | CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 | ||
| Formula | C17H14O4S | M.Wt | 314.36 |
| Solubility | ≥ 15.72mg/mL in DMSO | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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