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Comparison of Solubility, Plasma Protein Binding, and Transporter Inhibition
| Solubility in PBS pH 7.4 (μM) | Human plasma protein binding (fraction unbound) (%) | OATP1B1 IC50 (μM) | OATP1B3 IC50 (μM) | MRP2 IC50 (μM) | Pgp IC50 (μM) | BSEP IC50 (μM) | |
|---|---|---|---|---|---|---|---|
| CsA | 36 | <1 | 0.85 | 0.13 | 4.1 | 0.73 | 0.46 |
| Alisporivir | 15 | <4 | 0.45 | 0.19 | ∼16 (>49%) | 0.72 | 0.18 |
| BC544 | 330 | 28 | 10.97 | 5.40 | >50 | >50 | 29.3 |
| NVP018 | 140 | 22 | 4.31 | 1.75 | >50 | >50 | 12.3 |
