A cell-permeable, bioavailable 2-trifluoromethyl analog of Indomethacin that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2, IC50 = 267 and 388nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC50 >100uM). Interacts with human COX-2 with much greater affinity than indomethacin (KI = 1.5 vs 13uM) and blocks COX-2 dependent arachidonic acid oxygenation (IC50 = 150nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC50 = 1.7mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10mg/kg). Primary Target: COX-2 Primary Target IC50: 267 and 388nM for mouse and human COX-2, respectively. Solubility: DMSO Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity:
~98% (HPLC)
Form:
Supplied as a white powder.
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