Biochem/physiol Actions

Reversible: no

Primary TargetCOX-2

Product does not compete with ATP.

Cell permeable: yes

Target IC₅₀: 3.8 µM against COX-2

General description

A cell-permeable, selective inhibitor of cyclooxygenase-2 (COX-2) in vitro. Inhibits sheep placenta COX-2 (IC₅₀ = 3.8 µM) while COX-1 activity is completely unaffected at concentrations up to 100 µM. Displays potent anti-inflammatory and analgesic activity in vivo in rat at concentrations of 0.3 to 5 mg/kg. Does not produce any significant gastrointestinal lesions even at single oral doses of 1000 mg/kg. A useful tool to explore the role of COX-2 in physiologic and pathophysiologic processes.

A cell-permeable selective inhibitor of COX-2 in vitro. Inhibits sheep placental COX-2 (IC₅₀ = 3.8 µM) while COX-1 activity is unaffected at concentrations up to 100 µM. Displays potent anti-inflammatory and analgesic activity in vivo in rat at concentrations from 0.3 to 5 mg/kg.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ouellet, M., and Percival, M.D. 1995. Biochem. J.306, 247.Futaki, N., et al. 1994. Prostaglandins47, 55.Arai, I., et al. 1993. Res. Comm. Chem. Pathol. Pharmacol.81, 259.Futaki, N., et al. 1993. Gen. Pharmacol.24, 105.Futaki, N., et al. 1993. J. Pharm.Pharmacol.45, 753.

Packaging

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Warning

Toxicity: Standard Handling (A)