Cholestatic potential of different compounds in the in vivo rat model and corresponding in vitro inhibitory effects on Bsep
| Compound | In vivo effect on plasma bile acids after intravenous administration to rats | In vitro inhibition of taurocholate transport in cLPMV | ||
|---|---|---|---|---|
| ED50 | Δ10 min | Δ30 min | ||
| mg/kg | μM | μM | ||
| Cyclosporin A | 14 | 115 | 100 | IC50 = 0.8 ± 0.23 |
| Glibenclamide | 17 | 10 | 5 | IC50 = 8.6 ± 1.9 |
| Troglitazone | 7.7 | 53 | 60 | K i = 1.3 ± 0.3 |
| Troglitazone sulfate | K i = 0.23 ± 0.09 | |||