O-Desmethyl | N-Desalkyl | 6-OH | Fluorophenyl-OH | Methoxy-Phenyl-OH | ||
---|---|---|---|---|---|---|
CYP4F12 AST | Km | 0.16 ± 0.01 | 231.3 ± 44.3 | 0.63 ± 0.13 | 2.27 ± 0.33 | Not formed by CYP4F12 |
Vmax | 4.2 ± 0.14 | 0.21 ± 0.03 | 0.04 ± 0.002 | 0.0003 ± 0.00008 | ||
Ki | 11.8 ± 1.7 | N.D. | N.D. | N.D. | ||
V/K | 26.3 | 9.1e-4 | 0.064 | 1.3e-4 | ||
CYP4F12 d3-AST | Km | 0.18 ± 0.03 | 200.5 ± 14.4 | 0.47 ± 0.09 | 2.54 ± 0.36 | Not formed by CYP4F12 |
Vmax | 0.67 ± 0.02 | 0.19 ± 0.01 | 0.03 ± 0.001 | 0.0003 ± 0.00007 | ||
Ki | N.D. | N.D. | N.D. | N.D. | ||
V/K | 3.72 | 9.5e-4 | 0.063 | 1.2e-4 | ||
H/D | 7.1 | 0.96 | 1.02 | 1.11 | N.D. | |
CYP3A4 AST | Km | 0.28 ± 0.09 | 200.4 ± 41.1 | 0.72 ± 0.06 | 155.6 ± 38.7 | 18.5 ± 3.3 |
Vmax | 0.44 ± 0.05 | 0.19 ± 0.04 | 0.19 ± 0.005 | 0.29 ± 0.05 | 0.001 ± 0.0005 | |
Ki | N.D. | N.D. | N.D. | N.D. | N.D. | |
V/K | 1.57 | 9.5e-4 | 0.26 | 0.0017 | 5.4e-5 | |
CYP3A4 d3-AST | Km | 0.34 ± 0.15 | 196.6 ± 33.3 | 0.64 ± 0.09 | 146.0 ± 20.8 | 24.6 ± 5.6 |
Vmax | 0.14 ± 0.02 | 0.18 ± 0.03 | 0.20 ± 0.05 | 0.54 ± 0.05 | 0.003 ± 0.0003 | |
Ki | N.D. | N.D. | N.D. | N.D. | ||
V/K | 0.41 | 9.2e-4 | 0.31 | 0.0036 | 1.2e-4 | |
H/D | 3.8 | 1.03 | 0.8 | 0.47 | 0.45 |
N.D., not determined.