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 4°C. For long-term storage, aliquot and store at 4°C. 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.
