Kinetic parameters of glycosidation for Compound A and UDP-sugars in human liver microsomes at pH 6.0 and 7.4
Cosubstrate | pH | Parameter | Glucuronidation | Glucosidation | Galactosidation |
|---|---|---|---|---|---|
| Compound A | 6.0 | K m (Compound A) | 6.0 ± 0.5 | 8.12 ± 1.40 | 20.7 ± 2.0 |
| V max | 1348 ± 29 | 642 ± 34 | 10.8 ± 0.5 | ||
| 7.4 | K m (Compound A) | 11.3 ± 0.6 | 18.0 ± 1.64 | 24.6 ± 4.4 | |
| V max | 1323 ± 25 | 649 ± 25 | 5.4 ± 0.5 | ||
| UDP-sugar | 6.0 | K m (UDP-sugar) | 28 ± 3 | 104 ± 10 | 1250 ± 190 |
| V max | 1051 ± 14 | 652 ± 7 | 4.92 ± 0.37 | ||
| 7.4 | K m (UDP-sugar) | 761 ± 42 | 543 ± 20 | 1305 ± 90 | |
|
|
|
V
max
| 1040 ± 18 | 551 ± 9 | 2.74 ± 0.09 |