Apparent kinetic parameters of raloxifene glucuronidation to M1 and M2 in human kidney, intestinal, and liver microsomes and calculated microsomal intrinsic and tissue intrinsic clearances
Data are presented as mean (S.E.).
| Vmax | Km | Ksi | Clint | Clint,o | |
|---|---|---|---|---|---|
| nmol · min−1 · mg−1 | μM | μl · min−1 · mg−1 | ml · min−1 · kg−1 | ||
| M1 | |||||
| HKM | 0.38 (0.07) | 130.0 (0.13) | n.d. | 2.9 (0.15) | 0.58 (0.15) |
| HIM | 0.40 (0.02) | 8.55 (0.15) | n.d. | 47.3 (0.15) | 4.25 (0.15) |
| HLM | 2.17 (0.06) | 161.0 (0.11) | n.d. | 13.5 (0.12) | 12.12 (0.12) |
| M2 | |||||
| HKM | 1.09 (0.22) | 75.9 (0.31) | 79.6 (0.31) | 14.4 (0.38) | 2.84 (0.38) |
| HIM | 2.21 (0.05) | 8.34 (0.17) | 470.1 (0.21) | 265.0 (0.17) | 23.8 (0.17) |
| HLM | 3.21 (0.15) | 105.0 (0.22) | 355 (0.37) | 30.6 (0.27) | 27.5 (0.27) |
HKM, human kidney microsomes; HIM, intestinal microsomes; HLM, liver microsomes; n.d., not determined.