Kinetic values for induction of the CYP3A4 reporter gene by putative CYP3A4 inducers
| Compound | hGR/hPXR Co-Transfected | Imax(SCE) | EC50 | IA |
|---|---|---|---|---|
| μM | SCE/μM | |||
| CPA | − | 9.0 ± 0.2 | 17.7 ± 1.0 | 0.5 |
| CPA | + | 11.2 ± 0.2 | 1.6 ± 0.2 | 6.9 |
| Clotrimazole | − | 8.6 ± 0.4 | 6.2 ± 1.1 | 1.4 |
| Clotrimazole | + | 15.2 ± 0.3 | 1.1 ± 0.1 | 14.0 |
| Fexofenadine | − | 17.9 ± 2.8 | 7.0 ± 4.4 | 2.6 |
| Fexofenadine | + | 47.0 ± 0.9 | 2.4 ± 0.3 | 19.8 |
| Lovastatin | − | DNF | ||
| Lovastatin | + | DNF | ||
| PCN | − | 13.2 ± 1.1 | 4.5 ± 1.9 | 2.9 |
| PCN | + | 44.3 ± 2.5 | 2.5 ± 0.8 | 17.7 |
| Pioglitazone | − | 12.5 ± 2.5 | 6.0 ± 5.3 | 2.1 |
| Pioglitazone | + | 31.2 ± 0.8 | 1.1 ± 0.2 | 28.4 |
| Pravastatin | − | NI | ||
| Pravastatin | + | NI | ||
| Simvastatin | − | 31.3 ± 4.8 | 17.4 ± 7.3 | 1.8 |
| Simvastatin | + | 81.5 ± 8.3 | 0.8 ± 0.6 | 100.5 |
| Sulfinpyrazole | − | 19.6 ± 1.7 | 15.7 ± 3.9 | 1.3 |
| Sulfinpyrazole | + | 13.9 ± 2.8 | 7.9 ± 6.1 | 1.8 |
| Troglitazone | − | DNF | ||
| Troglitazone | + | DNF |
Imax, EC50, and IA values were derived from concentration response curves for each compound. Four xenobiotic concentrations (1, 10, 30, and 50 μM) were used in the construction of each curve, and each data point was derived from eight replicates in a representative experiment. Imax, EC50, and IA values were only derived if the curve fitting passed strict criteria, as described under Materials and Methods.
NI, no statistically significant induction observed at any dose; DNF, data did not fit criteria for calculation ofImax, EC50, and IA values, as described under Materials and Methods.