TABLE 1

Kinetic parameters for gemcabene glucuronidation in human liver microsomes and recombinant UGT1A3, recombinant UGT2B7, and recombinant UGT2B17

Values are mean ± standard deviation of three experiments. HLM and recombinant UGTs were pretreated with alamethacin (50 μg/mg protein) and incubated with varying concentrations of gemcabene to determine kinetic parameters as described under Materials and Methods. The data were fitted to the Hill equation (S50).


Matrix

S50

Vmax

Hill Coefficient
mM nmol/mg/min n
HLM 1.37 ± 0.12 6.04 ± 0.38 1.8 ± 0.2
UGT1A3 0.92 ± 0.06 0.38 ± 0.02 2.4 ± 0.3
UGT2B7 1.45 ± 0.39 1.44 ± 0.27 1.6 ± 0.3
UGT2B17
1.37 ± 0.10
0.13 ± 0.01
2.4 ± 0.3