General description
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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
COX-2
Product does not compete with ATP.
Reversible: no
Target IC50: 3.8 µM against COX-2
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51143206
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 349254-5MG