Table 5.
In vitro ADME properties for representative analogue (compound 34).a
| Compound | aq. Kinetic sol. (PBS @ pH 7.4) | Caco-2 (Papp 10-6 m/s @ pH 7.4) | efflux ratio (B→A)/(A→B) | mouse liver microsome stability (T1/2) | PBS-pH 7.4 stability:% remaining after 48h | Mouse plasma stability:% remaining after 48h |
|---|---|---|---|---|---|---|
| 34 | 14.5 μM | 8.8 | 2.3 | <10 min. | 100 | 98.3 |
a
Kinetic solubility measurements were conducted at Analiza Inc. using nitrogen detection methodologies. Caco-2 permeability, microsomal stability and mouse plasma stability experiments were conducted at Pharmaron Inc.