IC50 values for the inhibition of UGT-mediated hydroxymidazolam glucuronidation by the UGT isoform-selective inhibitor or substrate in pooled HLMs
| UGT Isoform | Inhibitor | IC50 Valuesa | |||
|---|---|---|---|---|---|
| 1′-Hydroxymidazolam N-glucuronide | 1′-Hydroxymidazolam O-glucuronide | 4-Hydroxymidazolam Glucuronide I | 4-Hydroxymidazolam Glucuronide II | ||
| μM | |||||
| 1A4 | Hecogenin | 1.5 | >5 | 0.8 | >5 |
| 2B7 | Diclofenac | 802.8 | 2.0 | 941.1 | 46.6 |
↵a Averages of duplicate determinations.