Table 1. Kinetic values for tolbutamide activities of recombinant wild-type and mutant CYP2C9 proteins.
Allelic protein | Vmax (pmol·min−1·pmol−1 P450) | Km (μmol/L) | Clearance (Vmax/Km) | Relative clearance*/.1 |
---|---|---|---|---|
CYP2C9.36 | 17.45±0.89b | 74.82±14.46b | (2.33±0.31)E-01b | 237.15%b |
CYP2C9.51 | 8.44±0.30b | 54.17±8.13 | (1.56±0.33)E-01b | 158.50%b |
N418T | 5.86±0.25b | 57.31±10.00 | (1.02±0.18)E-01 | 104.02% |
CYP2C9.11 | 5.02±0.11 | 50.24±4.78 | (1.00±0.12)E-01 | 101.64% |
CYP2C9.1 | 4.70±0.10 | 47.74±4.57 | (9.83±0.48)E-02 | 100.00% |
CYP2C9.56 | 5.25±0.19 | 55.71±8.44 | (9.43±1.89)E-02 | 95.86% |
CYP2C9.46 | 5.46±0.29 | 82.94±16.13b | (6.58±0.11)E-02b | 66.88%b |
CYP2C9.53 | 3.73±0.08b | 59.98±5.55b | (6.21±0.03)E-02b | 63.17%b |
CYP2C9.44 | 3.21±0.06b | 52.81±4.44 | (6.08±0.29)E-02b | 61.85%b |
CYP2C9.41 | 3.22±0.14b | 54.08±10.25 | (5.95±0.72)E-02b | 60.51%b |
CYP2C9.54 | 7.40±0.31b | 138.20±18.36b | (5.35±0.51)E-02b | 54.42%b |
CYP2C9.29 | 2.69±0.08b | 52.00±6.32 | (5.17±0.20)E-02b | 52.60%b |
CYP2C9.27 | 2.92±0.08b | 59.23±6.47b | (4.92±0.89)E-02b | 50.08%b |
CYP2C9.38 | 3.42±0.15b | 69.77±11.85b | (4.89±0.12)E-02b | 49.77%b |
CYP2C9.2 | 5.73±0.29 | 123.30±20.18b | (4.65±0.54)E-02b | 47.24%b |
CYP2C9.40 | 3.36±0.11b | 74.07±9.27b | (4.53±0.09)E-02b | 46.08%b |
CYP2C9.55 | 6.97±0.34b | 169.50±24.40b | (4.11±0.07)E-02b | 41.80%b |
CYP2C9.47 | 6.32±0.48b | 168.30±37.76b | (3.75±0.63)E-02b | 38.16%b |
CYP2C9.34 | 1.61±0.05b | 45.61±6.03 | (3.52±0.35)E-02b | 35.80%b |
CYP2C9.31 | 1.85±0.05b | 54.71±6.15 | (3.38±0.41)E-02b | 34.40%b |
CYP2C9.48 | 7.21±0.43b | 217.30±36.12b | (3.32±0.58)E-02b | 33.76%b |
CYP2C9.49 | 2.71±0.15b | 95.14±18.46b | (2.85±0.09)E-02b | 28.96%b |
CYP2C9.37 | 5.10±0.34 | 236.50±42.23b | (2.15±0.23)E-02b | 21.91%b |
CYP2C9.50 | 8.19±0.73b | 383.00±79.38b | (2.14±0.47)E-02b | 21.75%b |
CYP2C9.8 | 1.37±0.04b | 68.29±7.59b | (2.00±0.49)E-02b | 20.32%b |
CYP2C9.14 | 0.97±0.03b | 51.68±6.91 | (1.87±0.26)E-02b | 19.03%b |
CYP2C9.23 | 1.43±0.04b | 82.01±9.23b | (1.74±0.19)E-02b | 17.67%b |
CYP2C9.45 | 0.64±0.03b | 54.66±11.38 | (1.17±0.050)E-02b | 11.90%b |
CYP2C9.3 | 2.94±0.27b | 271.00±63.38b | (1.08±0.097)E-02b | 11.02%b |
CYP2C9.16 | 0.11±0.0017b | 11.65±1.29b | (9.11±0.15)E-03b | 9.26%b |
CYP2C9.42 | 0.48±0.02b | 122.20±20.44b | (3.94±0.92)E-03b | 4.01%b |
CYP2C9.39 | 0.49±0.02b | 126.40±17.08b | (3.89±0.46)E-03b | 3.95%b |
CYP2C9.52 | 0.25±001b | 94.72±12.41b | (2.66±0.51)E-03b | 2.70%b |
CYP2C9.13 | 0.13±0.01b | 496.70±83.74b | (2.57±0.64)E-04b | 0.26%b |
CYP2C9.43 | 0.06±0.0040b | 250.90±43.97b | (2.42±0.42)E-04b | 0.25%b |
CYP2C9.33 | 0.04±0.0027b | 193.60±41.46b | (1.84±0.17)E-04b | 0.19%b |
CYP2C9.19 | 0.06±0.01b | 827.00±151.70b | (7.74±0.89)E-05b | 0.08%b |
b Represent P<0.05 vs wild-type.
* Relative clearance value to wild-type.