Rofecoxib

Catalog No.S3043 Synonyms: MK-0966

Rofecoxib Chemical Structure

Molecular Weight(MW): 314.36

Rofecoxib is a COX-2 inhibitor with IC50 of 18 nM.

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In DMSO USD 130 In stock
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Cited by 1 publication

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Biological Activity

Description Rofecoxib is a COX-2 inhibitor with IC50 of 18 nM.
Targets
COX-2 [1]
18 nM
In vitro

Rofecoxib inhibits the COX-2-dependent production of PGE2 in human osteosarcoma cells with an IC50 of 26 nM. Rofecoxib is a time-dependent inhibitor of purified human recombinant COX-2 with an IC50 of 0.34 μM. Rofecoxib causes inhibition of purified human COX-1 in a non-time-dependent manner. In a human whole blood assay, Rofecoxib selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE2 synthesis with an IC50 value of 0.53 μM compared with an IC50 value of 18.8 μM for the inhibition of COX-1-derived thromboxane B2 synthesis after blood coagulation. [1] Rofecoxib moderately inhibits phenacetin O-deethylation with an IC50 of 23 μM. And a 30-minute preincubation with microsomes and NADPH considerably increases the inhibitory effect of Rofecoxib with an IC50 of 4.2 μM. Inactivation of CYP1A2 by rofecoxib requires NADPH, and is characterized by a K i of 4.8 μM. [2]

In vivo Rofecoxib potently inhibits carrageenan-induced paw edema, carrageenan-induced paw hyperalgesia, lipopolysaccharide-induced pyresis with IC50 of 1.5 mg/kg, 1.0 mg/kg and 0.24 mg/kg, respectively. Rofecoxib also blocks adjuvant-induced arthritis with an IC50 of 0.74 mg/kg/day. Rofecoxib also has a protective effect on adjuvant-induced destruction of cartilage and bone structures in rats. [1] Oral administration of rofecoxib decreases portal pressure in rats that are treated with CCl4 for 8 weeks. In addition, rofecoxib administration reduces the number of activated HSCs and to downregulate hepatic protein levels of three detected types of collagen, laminin, VEGF and CTGF in CCl4-treated rats. [3]

Protocol

Kinase Assay:[1]
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In vitro biochemical and pharmacological assaysinhibition studies with recombinant human COX-1 and COX-2:

Microsomal preparations of recombinant human COX-1 and COX-2 are prepared from a vaccinia virus-COS-7 cell expression system. Recombinant human COX-1 and COX-2 are expressed in baculovirus-Sf9 cells, and enzymes are purified. Enzymatic activity is monitored continuously by either a fluorescence assay measuring the appearance of the oxidized form of the reducing agent cosubstrate homovanillic acid or by oxygen consumption. The HPLC assay for the assessment of inhibition of purified COX-1 by Rofecoxib with 0.1 μM arachidonic acid substrate concentration, the determination of the stoichiometry of the complex between COX-2 and Rofecoxib, the dissociation rate constant of the enzyme-inhibitor complex by recovery of enzymatic activity, and the recovery of intact Rofecoxib from that complex are all performed as described previously. The solvent system for the HPLC analysis of Rofecoxib is 15:85 MeOH/aqueous potassium phosphate (1 g/liter), with elution by a linear gradient of 15 to 75% MeOH over 25 minutes with detection at 275 nm on a Novapak C18 column.
Cell Research:[1]
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  • Cell lines: Human osteosarcoma cell line and human lymphoma U937 cells
  • Concentrations: 0.5 μM, 8 μM
  • Incubation Time: 15 minutes
  • Method: The human osteosarcoma cell line has been shown to selectively express COX-2 by reverse transcription-polymerase chain reaction and immunoblot analysis, whereas undifferentiated human lymphoma U937 cells selectively express COX-1. The production of PGE2 by these cells after arachidonic acid challenge is used as an index of cellular COX-2 and COX-1 activity, respectively. Rofecoxib is preincubated for 5 to 15 minutes with the cells under serum-free conditions [Hanks' balanced salt solution (HBSS)] before a 10-minutes stimulation with 10 μM arachidonic acid and measurement of PGE2 production. COX activity in each cell line is defined as the difference in PGE2 concentrations in samples incubated in the presence or absence of arachidonic acid.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Rat adjuvant-induced arthritis (AIA) model
  • Formulation: 80% PEG 200 in distilled water
  • Dosages: 0.1 mg/kg/day, 0.3 mg/kg/day, 1.0 mg/kg/day, and 3.0 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (200.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.36
Formula

C17H14O4S
CAS No. 162011-90-7
Storage powder
in solvent
Synonyms MK-0966

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00165048 Unknown status Cancer of Stomach Chinese University of Hong Kong October 2004 Phase 3
NCT00164892 Unknown status Cancer of Stomach Chinese University of Hong Kong October 2004 Phase 3
NCT00165048 Unknown status Cancer of Stomach Chinese University of Hong Kong October 2004 Phase 3
NCT00164892 Unknown status Cancer of Stomach Chinese University of Hong Kong October 2004 Phase 3
NCT00263094 Completed Headache Sheba Medical Center September 2004 Not Applicable
NCT00263094 Completed Headache Sheba Medical Center September 2004 Not Applicable

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID