Indomethacin, 2′-Trifluoromethyl

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).

Cell permeable: yes

Primary Target
COX-2

Reversible: yes

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

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)