1. Immunology/Inflammation
  2. COX
  3. Rofecoxib

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).

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Rofecoxib Chemical Structure

Rofecoxib Chemical Structure

CAS No. : 162011-90-7

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Based on 3 publication(s) in Google Scholar

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  • Biological Activity

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  • References

  • Customer Review

Description

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).

IC50 & Target[1]

Human COX-2

18 nM (IC50, in Chinese hamster ovary cells)

Human COX-2

26 nM (IC50, in human osteosarcoma cells)

In Vitro

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[1]. 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[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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[1]. 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

314.36

Formula

C17H14O4S

CAS No.
Appearance

Solid

Color

Light yellow to green

SMILES

O=C1OCC(C2=CC=C(S(=O)(C)=O)C=C2)=C1C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (106.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

References
Cell Assay
[3]

The anti-proliferative activity of single drug treatments is assessed in a monolayer culture condition by plating Ist-Mes-1, Ist-Mes-2 and MPP89 cells in T25 flask. After 24 h, DMSO (at the same final concentration of that present in medium with drugs), 50 μM gefitinib or 36 μM Rofecoxib are added. The cells are then harvested at 48 h after treatment and analyzed by western blot and RT-PCR to evaluate the effect of the drugs on expression and mRNA levels of EGFR and COX-2. The expression of the cell cycle arrest genes and p-AKT, AKT, p-ERK and ERK is detected by Western blot to assess the antiproliferative activity of the two drugs in isolation (25 μM gefitinib or 4 μM Rofecoxib) and in combination 25 μM gefitinib+4 μM Rofecoxib[3].

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

Animal Administration
[2]

Mice[2]
Retinopathy of prematurity (ROP) is induced in C57BL/6J mice. The mice are randomly allocated into three experimental groups with 16 mice in each group: normal group-age-matched mice are maintained in room air from birth to P17 and are served as negative control; untreated ROP group-ROP is induced as described above without treatment and served as positive control; Rofecoxib-treated ROP group-ROP mice are treated daily with Rofecoxib (15 mg/kg body weight, intraperitoneally) from P12 to P17. Rofecoxib is dissolved in a 0.5% aqueous methylcellulose solution before administration[2].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1811 mL 15.9053 mL 31.8107 mL 79.5267 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 mL 15.9053 mL
10 mM 0.3181 mL 1.5905 mL 3.1811 mL 7.9527 mL
15 mM 0.2121 mL 1.0604 mL 2.1207 mL 5.3018 mL
20 mM 0.1591 mL 0.7953 mL 1.5905 mL 3.9763 mL
25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1811 mL
30 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6509 mL
40 mM 0.0795 mL 0.3976 mL 0.7953 mL 1.9882 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7953 mL
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Rofecoxib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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