TABLE 1

Kinetic analyses for imrecoxib oxidation, M1 oxidation, M-CHO oxidation, and reduction in HLMs, HLCs, or NADPH-fortified HLCs

SubstrateMetaboliteIncubationProtein ConcentrationIncubation TimeConcentration RangeVmaxKmIntrinsic Clearance
mg/mlminμMpmol/min per mg proteinμMμl/min per mg protein
ImrecoxibM1HLM (NADPH)0.02600.01–1002963.7279.6
M1M-CHOHLM (NADPH)0.10600.25–25001379790.140
M1M-CHOHLC0.10600.25–250033.912990.0261
M-CHOM1HLM (NADPH)0.04450.01–1007258.0190.5
M-CHOM2HLM (NADPH)0.04450.01–100278056.948.9
M-CHOM2HLC0.04450.01–302091.30161
M-CHOM1HLC (NADPH)0.02100.01–1009731.34727
M-CHOM2HLC (NADPH)0.02100.01–10039,19543091.2