Kinetic analysis of 4′-OH-diclofenac and E-3174 formation by recombinant CYP2C9 variants expressed in yeast
| CYP2C9 variants | Vmax | Km | Vmax/Km |
|---|---|---|---|
| nmol/min/nmol P450 | μM | ml/min/nmol P450 | |
| Diclofenac → 4′-OH diclofenac | |||
| CYP2C9.1 | 25.1–26.5 | 7.0–7.7 | 3.4–3.6 |
| CYP2C9.2 | 11.1–11.8 | 5.0–6.1 | 1.9–2.2 |
| CYP2C9.3 | 25.2–28.7 | 22.1–26.4 | 1.1–1.1 |
| Losartan → E-3174 | |||
| CYP2C9.1 | 0.83–0.92 | 4.75–5.80 | 0.159–0.175 |
| CYP2C9.2 | 0.44–0.37 | 3.84–3.62 | 0.103–0.115 |
| CYP2C9.3 | 0.20–0.12 | 6.78–6.61 | 0.018–0.029 |
Data are presented as the range of two means obtained in two independent experiments.