Michaelis-Menten parameters for the cellular uptake of bosentan and Ro 48-5033 into human OATP-expressing CHO cells
Substrate | Transporter | Km | Vmax | Vmax/Km |
|---|---|---|---|---|
| μM | pmol/min · μg protein | μl/min · μg | ||
| Bosentan | OATP1B3 | 141 ± 17 | 3.21 ± 0.40 | 0.023 |
| OATP1B1 | 44 ± 5 | 1.32 ± 0.05 | 0.030 | |
| OATP2B1 | 202 ± 107 | 2.27 ± 0.69 | 0.011 | |
| Ro 48-5033 | OATP1B3 | 166 ± 16 | 2.14 ± 0.32 | 0.013 |
| OATP1B1 | 60 ± 17 | 0.89 ± 0.08 | 0.015 | |
|
| OATP2B1 |
a
|
|
|
↵ a No transport detectable for Ro 48-5033.