Metabolism and uptake CLint,in vitro determinations for an AZ project compound
| Species | Metabolic CLint,in vitro | Uptake CLint,in vitro | |||
|---|---|---|---|---|---|
| Microsomes | Fresh Hepatocytes | Cryopreserved Hepatocytes | Fresh Hepatocytes | Cryopreserved Hepatocytes | |
| μl/min/mg | μl/min/106 cells | ||||
| Rat | 10 ± 2 | 44 ± 5 | 11 ± 3*** | 432 ± 53 | 204 ± 31** |
| Human | 12 ± 3 | N.D. | <5a | N.D. | 96 ± 22 |
Metabolic stability and uptake (loss from media method) curves are shown in Fig. 7. Data represent mean 6 S.D.; n = 3. **P, 0.01; ***P, 0.001 vs. fresh hepatocytes.
N.D., not determined.
↵a <5 μl/min/106 hepatocytes, below the detection limit of the assay.