Cat. No.: HY-17372

Rofecoxib

(Synonyms: MK 966)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

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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Pureté: 99.89%
CAS No.: 162011-90-7
Formule: C₁₇H₁₄O₄S
Masse moléculaire:314.36

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rofecoxib Chemical Structure

CAS No.: 162011-90-7

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Human COX-2

18 nM (IC₅₀, in Chinese hamster ovary cells)

Human COX-2

26 nM (IC₅₀, in human osteosarcoma cells)

Voir tous les produits spécifiques à Isoform COX :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.02 μM Compound: 1 (MK-966)	In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells. In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells.	[PMID: 10197970]
CHO	IC₅₀	0.02 μM Compound: 1 (Rofecoxib)	Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells. Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells.	[PMID: 12643942]
CHO	IC₅₀	0.02 μM Compound: Rofecoxib	In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells	[PMID: 10576684]
CHO	IC₅₀	0.02 μM Compound: Rofecoxib	Inhibition of PGE-2 production in CHO cells expressing human COX-2. Inhibition of PGE-2 production in CHO cells expressing human COX-2.	[PMID: 10576685]
CHO	IC₅₀	18 μM Compound: MK 966; Vioxx(R)	Inhibition of human COX2 expressed in CHO cells cells assessed as reduction in PGE2 release Inhibition of human COX2 expressed in CHO cells cells assessed as reduction in PGE2 release	[PMID: 30909021]
DU-145	IC₅₀	200 μM Compound: 2, Rofecoxib, MK 966, VIOXX	Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay	[PMID: 23735281]
J774	IC₅₀	>10 μM Compound: rofecoxib	In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells	[PMID: 15857149]
J774	IC₅₀	0.012 μM Compound: rofecoxib	In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells	[PMID: 15857149]
PC-3	IC₅₀	>50 μM Compound: 2, Rofecoxib, MK 966, VIOXX	Antiproliferative activity against human PC3 cells expressing PCDNA after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells expressing PCDNA after 72 hrs by MTT assay	[PMID: 23735281]
PC-3	IC₅₀	>50 μM Compound: 2, Rofecoxib, MK 966, VIOXX	Antiproliferative activity against human PC3 cells expressing SKP2 after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells expressing SKP2 after 72 hrs by MTT assay	[PMID: 23735281]
PC-3	IC₅₀	200 μM Compound: 2, Rofecoxib, MK 966, VIOXX	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 23735281]
Sf21	IC₅₀	0.12 μM Compound: rofecoxib	Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay	[PMID: 17378609]
Sf21	IC₅₀	0.156 μM Compound: 1,A, Vivoxx	Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 5 mins by EIA Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 5 mins by EIA	[PMID: 21752640]
Sf21	IC₅₀	0.17 μM Compound: 2	Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as conversion of arachidonic acid to PGE2 preincubated for 15 mins measured after 5 mins by enzyme immunoassay Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as conversion of arachidonic acid to PGE2 preincubated for 15 mins measured after 5 mins by enzyme immunoassay	[PMID: 21958737]
Sf21	IC₅₀	0.17 μM Compound: Rofecoxib	Inhibition of human recombinant COX2 expressed in Sf21 cells using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 5 mins Inhibition of human recombinant COX2 expressed in Sf21 cells using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 5 mins	[PMID: 22652053]
Sf21	IC₅₀	74.5 nM Compound: Rofecoxib	Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as effect on prostaglandin E2 production by ELISA Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as effect on prostaglandin E2 production by ELISA	[PMID: 19056264]
Sf9	IC₅₀	107 nM Compound: Rofecoxib	Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay	[PMID: 19520573]
U-937	IC₅₀	>10 μM Compound: 3 (rofecoxib)	In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells	[PMID: 12877584]
U-937	IC₅₀	2 μM Compound: Rofecoxib	Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes.	[PMID: 10576685]

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 162011-90-7
Appearance Solid
Masse moléculaire 314.36
Formule C₁₇H₁₄O₄S
Color White to yellow
SMILES

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

MK 966
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Br J Pharmacol

Assessment of the molecular mechanisms of drug-induced hidden cardiotoxicity by a multi-omics approach: The example of rofecoxib. [Abstract]

2025 Jun 18. PMID: 40532721
Biochem Pharmacol

Chronic treatment with rofecoxib but not ischemic preconditioning of the myocardium ameliorates early intestinal damage following cardiac ischemia/reperfusion injury in rats. [Abstract]

2020 Aug:178:114099. PMID: 32540483
Cells

Lack of Small Intestinal Dysbiosis Following Long-Term Selective Inhibition of Cyclooxygenase-2 by Rofecoxib in the Rat. [Abstract]

2019 Mar 15;8(3):251. PMID: 30884758
J Pharmacol Exp Ther

Disulfiram activation of prostaglandin E2 synthesis: a novel antifibrotic mechanism in pulmonary fibrosis. [Abstract]

2025 Jun;392(6):103588. PMID: 40359874
Res Sq

2026 Apr 3.
Asian Pac J Cancer Prev

Antitumour Activities of Selected Pure Compounds Identified from the Serum of Crocodylus porosus, Malayopython reticulatus, Varanus salvator and Cuora kamaroma amboinensis. [Abstract]

2021 Feb 12;22(S1):97-106. PMID: 33576218

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

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Molecular Weight Molecular Weight

Calculateur de dilution

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

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In Vivo:

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

Stock Solution Working Solution

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:

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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).

Working solution concentration: 0.22 mg/mL

Protocole

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].

MedChemExpress (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].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (289 KB)
SDS (392 KB)
- English - EN (392 KB)
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- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[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. [Content Brief]

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Rofecoxib

6 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Rofecoxib

Voir tous les produits spécifiques à Isoform COX

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Rofecoxib Related Classifications

HY-17372 Related Classifications