Table 2. Physicochemical Properties Determined for the Cyclopeptides.
cyclopeptide | Log D, pH 7.0a | solubility PBS, pH 7.4/pH 1.0 (μM)b | PAMPA (Pe × 10–6 cm/s)c |
---|---|---|---|
2 | 5.8 | 0.94/1.17 | 0.6 |
3 | 6.0 | 0.38/3.46 | 1.0 |
4 | 3.7 | 0.55/0.38 | 0.2 |
5 | 6.3 | 0.18/0.74 | 0.3 |
6 | 8.0 | 0.71/5.32 | 0.2 |
7 | 7.7 | 0.12/0.21 | 2.0 |
8 | 3.1 | nd | d |
9 | 3.7 | nd | e |
10 | 3.9 | 436.52/28.33 | 0.2 |
Measured (see Supporting Information).
Number of replicates, n = 2.
Number of replicates, n = 3; nd: not determined.
Compound was not detected in the acceptor compartment (lower limit of quantitation, LLOQ = 0.02 μM).
Compound was not detected in the acceptor compartment (lower limit of quantitation, LLOQ = 0.03 μM).