UGT enzyme activity inhibition results for irosustat and 667-coumarin
Results are mean values from triplicate incubations.
| UGT Enzyme | Activity | Direct IC50 (CV) | |
|---|---|---|---|
| Irosustat | 667-Coumarin | ||
| μM | |||
| UGT1A1 | 7-Hydroxy-4-methylcoumarin glucuronosyltransferase | 43 (9%) | 30 (9%) |
| UGT1A4 | Trifluoperazine glucuronosyltransferase | N.A. | >50 |
| UGT2B7 | 7-Hydroxy-4-methylcoumarin glucuronosyltransferase | >50 | ∼50 |
CV, coefficient of variation of the estimates; N.A., not assessed (no inhibition found at any of the assayed concentrations, up to 50 μM).