Biochem/physiol Actions

Reversible: yes

Primary TargetCOX-2

Target IC₅₀: 267 and 388 nM for mouse and human COX-2, respectively

Cell permeable: yes

General description

A cell-permeable, bioavailable 2′-trifluoromethyl analog of Indomethacin (>Cat. No. 405268) that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2; IC₅₀ = 267 and 388 nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC₅₀ >100 µM). Interacts with human COX-2 with much greater affinity than indomethacin (K_I = 1.5 vs 13 µM) and blocks COX-2 dependent arachidonic acid oxygenation (IC₅₀ = 150 nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC₅₀ = 1.7 mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10 mg/kg).

Legal Information

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

Other Notes

Blobaum, A.L., et al. 2013. ACS Med. Chem. Lett.4, 486.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)