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In Vitro ADME Profile of 1, 56 and 57.
| 1 | 56 | 57* | |
|---|---|---|---|
| Solubility at pH = 7.4 (μM) | 1.4 | 5.5 | 23 |
| PAMPA (1 × 10−6 cm/s) | 1232 | 316 | 413 |
| Caco2 Permeability (nm/s) | |||
| A/B | 161 | 243 | 302 |
| Plasma Protein Binding (%) | |||
| mouse | 99 | 92 | 92 |
| rat | 98 | 89 | 91 |
| human | 99 | 92 | 93 |
| Metabolic Stability (T1/2, min) | |||
| mouse | 16 | 113 | 8 |
| rat | 31 | 294 | 47 |
| human | 8 | 64 | 7 |
| Plasma Stability (T1/2, h) | >48 | >48 | >48 |
previously determined.8
