Table 4.
Aqueous solubility and stability and Caco-2 permeability data for selected agents.
| Analogue | Kinetic Solubiltya (μM) | Papp(A–B)b (10−6 cm/s) | Papp(B–A)b (10−6 cm/s) | 48 hr Aqueous Stabilityc (DPBS buffer, pH 7.4) |
|---|---|---|---|---|
| 45 | 4.3 | 25.5 | 12.7 | > 95% |
| 46 | 6.6 | 18.9 | 8.9 | > 95% |
| 54 | 143.3 | 35.4 | 23.1 | > 95% |
a
Solubility measurements done at Analiza, Inc. (http://analiza.com).
b
Caco-2 permeability was measured at Cyprotex (www.cyprotex.com/adme).
c
Aqueous stability measured over 48 h in pH 7.4 DPBS buffer.