Compound | Liver Microsome | Kinetic Parameter | |||
---|---|---|---|---|---|
Km | Vmax | Ki | CLint | ||
μM | nmol/min per mg | mM | µl/min per mg | ||
Etodolac | Humanized UGT1 micea | 483 ± 40 | 0.379 ± 0.003 | ― | 0.79 ± 0.06 |
Humansa | 483 ± 50 | 0.246 ± 0.012 | ― | 0.51 ± 0.03 | |
Micea | 1170 ± 287 | 0.201 ± 0.029 | ― | 0.17 ± 0.01 | |
Diclofenac | Humanized UGT1 micea | 31.8 ± 1.91 | 7.05 ± 0.04 | ― | 222 ± 12.2 |
Humansb | 33.1 ± 1.70 | 10.4 ± 0.28 | 22.5 ± 1.00 | 313 ± 8.88 | |
Micea | 55.6 ± 1.52 | 11.8 ± 0.10 | ― | 211 ± 5.62 | |
rac-Ibuprofen | Humanized UGT1 micea | 319 ± 26 | 4.27 ± 0.12 | ― | 13.4 ± 0.71 |
Humansa | 651 ± 8.1 | 6.44 ± 0.05 | ― | 9.9 ± 0.05 | |
Micea | 364 ± 12 | 11.2 ± 0.19 | ― | 30.7 ± 0.54 | |
S-Ibuprofen | Humanized UGT1 micea | 381 ± 26 | 7.54 ± 0.16 | ― | 19.9 ± 1.00 |
Humansa | 699 ± 34 | 8.71 ± 0.17 | ― | 12.5 ± 0.38 | |
Micea | 364 ± 5.0 | 16.5 ± 0.19 | ― | 45.1 ± 0.50 | |
R-Ibuprofen | Humanized UGT1 micea | 320 ± 38 | 2.18 ± 0.07 | ― | 6.87 ± 0.56 |
Humansa | 428 ± 11 | 3.37 ± 0.03 | ― | 7.86 ± 0.13 | |
Micea | 424 ± 19 | 8.00 ± 0.09 | ― | 18.9 ± 0.70 |