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Comparison of solubility, plasma protein binding and transporter inhibition
| Solubility in PBS pH7.4 (uM) |
Human PPB (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 |
