IC50 values for rosiglitazone, pioglitazone, and troglitazone against drug oxidation activities catalyzed by human hepatic microsomes
| Isoform | Rosiglitazone IC50 | Pioglitazone IC50 | Troglitazone IC50 |
|---|---|---|---|
| μM | |||
| CYP1A2 | 55.0 | NA | 23.4 |
| CYP2A6 | NA | NA | 24.6 |
| CYP2C8 | 9.58 | 9.38 | 2.33 |
| CYP2C9 | 83.2 | 100 | 2.73 |
| CYP2C19 | NA | 83.3 | 25.7 |
| CYP2D6 | 42.1 | NA | NA |
| CYP2E1 | NA | NA | NA |
| CYP3A4 | 28.0 | 12.3 | 14.5 |
Incubations were conducted with pooled human microsomes (n = 15) under conditions outlined underMaterials and Methods. The substrate probes were used at their in vitro Km values. A Micromass Quattro II or an LC tandem quadrupole mass spectrometer were used to monitor ions of the respective P450 marker metabolites
NA, no inhibition observed below 50%.