Table 2.
In vitro plasma stabilities of 11–14, 16 and 18–21 determined at 37 °C.
| Compd | % intact peptide in human plasma after the given incubation time | ||||||
|---|---|---|---|---|---|---|---|
| 10 min | 25 min | 1 h | 2 h | 6 h | 24 h | 48 h | |
| 11 | 72 ± 1 | 24 ± 1 | 1.1 ± 0.1 | < 1 | n.d | n.d | n.d |
| 12 | 86 ± 1 | 28 ± 1 | < 1 | < 1 | n.d | n.d | n.d |
| 13 | n.d | n.d | n.d | > 99 | > 99 | > 99 | 96 ± 1 |
| 14 | 50 ± 2 | n.d | < 1 | n.d | < 1 | < 1 | n.d |
| 16 | n.d | n.d | > 99 | n.d | > 99 | > 99 | > 99 |
| 18 | 59 ± 1 | n.d | < 1 | n.d | < 1 | < 1 | n.d |
| 19 | n.d | n.d | > 99 | n.d | > 99 | > 99 | 99 ± 1 |
| 20 | 78 ± 1 | n.d | 6.4 ± 0.1 | n.d | n.d | < 1 | n.d |
| 21 | n.d | n.d | > 99 | n.d | > 99 | > 99 | 99 ± 1 |
| Compd | % intact peptide in mouse plasma after the given incubation time | ||||||
|---|---|---|---|---|---|---|---|
| 10 min | 25 min | 1 h | 2 h | 6 h | 24 h | 48 h | |
| 21 | > 99 | n.d | > 99 | > 99 | > 99 | > 99 | > 99 |
The initial concentration of each peptide in human or mouse plasma/PBS (1:2 v/v) was 100 µM. Data represent mean values (± SEM) from three independent experiments (SEM not given when no decomposition was observed).