Table 5. Summary of In Vitro ADME Properties of 4, 5, 6, 7, 8, and 1.
aqueous
solubility (μM) |
|||||
---|---|---|---|---|---|
compound | pH 1.2 | pH 6.8 | PAMPA permeability (×10–6 cm/s) | hepatic microsome stability in rats (mL/min/kg) | plasma protein binding in rats (% unbound) |
4 | <0.02 | >100 | >50 | 171 | <0.01 |
5 | 0.054 | >100 | >50 | 237 | <0.01 |
6 | <0.01 | >100 | >50 | 275 | <0.01 |
7 | <0.02 | 89.5 | >50 | 123 | <0.01 |
8 | <0.01 | >100 | >50 | 296 | <0.01 |
1a | 0.088 | >100 | >50 | 38.7 | 0.51 |