TABLE 4
In vitro and in vivo correlation of Kpuu in WH rat and impact of BSA on Kpuu
| Compounds | In Vitro Kpuu Hepatocyte | In Vivo Kpuu IV Infusion | |||
|---|---|---|---|---|---|
| 0% BSA | 0.2% BSA | 2% BSA | 4% BSA | ||
PF-06649298
 | 4.6 ± 0.4 | 5.5 ± 0.7 | 9.5 ± 2.2 | 14 ± 2.6 | 16 ± 1.3 |
PF-06761281
 | 0.8 ± 0.1 | 1.0 ± 0.2 | 1.2 ± 0.3 | 1.5 ± 0.3 | 1.7 ± 0.4 |
PF-06741415
 | 1.0 ± 0.1 | 0.7 ± 0.03 | 0.5 ± 0.2 | 0.5 ± 0.2 | 2.4 ± 0.6 |
Kpuu was measured at hepatocyte cell density of 0.5 million cells/ml, 1 μM test compound concentration, and 4-hour incubation time.