Effects of R115866 on CYP-dependent activities
| Activities | Enzyme Source | CYP Isozyme | IC50 |
|---|---|---|---|
| μM | |||
| RA 4-hydroxylase | Yeast microsomes | CYP26 | 0.004 |
| Aromatase | Human placental microsomes | CYP19 | 2.6 |
| 17,20-Lyase | Rat testicular S10 fraction | CYP17 | 1.2 |
| Testosterone 2α-hydroxylase | Rat liver microsomes | CYP2C11 | 7.2 |
| Testosterone 6β-hydroxylase | Rat liver microsomes | CYP3A | 20% at 10 μM1-a |
| Testosterone 7α-hydroxylase | Rat liver microsomes | CYP2A1 | 9.1 |
↵1-a Expressed as percentage of inhibition at 10 μM.