Mean apparent kinetic parameters for the glucuronidation of MK-0524 with recombinant human UGT
MK-0524 (0.3–40 μM) was incubated with membrane preparations of recombinant human UGT from baculovirus-infected cells (0.1 mg/ml) in the presence of 2 mM UDPGA at 37°C. Values represent mean; n = 2.
Human UGT Isoform | App Vmax | App Km | App Vmax/Km |
|---|---|---|---|
| pmol/min/mg | μM | μl/min/mg | |
| UGT1A1 | 8 | 1.9 | 4 |
| UGT1A3 | 413 | 6.6 | 62 |
| UGT1A8 | N.D.a | N.D. | N.D. |
| UGT1A9 | 87 | 13.3 | 7 |
| UGT1A10 | N.D. | N.D. | N.D. |
| UGT2B7 | 106 | 3.3 | 32 |
↵ a N.D., not determined. No metabolite formation was observed.