The in vitro bioactivities and stabilities of 1a–1i.
Peptide | EC50a (nM) | Plasma half-lifeb (h) | Peptide | EC50a (nM) | Plasma half-lifeb (h) |
---|---|---|---|---|---|
Lixisenatide | 0.076 ± 0.013 | 7.1 | 1e | 0.13 ± 0.03 | 21.2 |
1a | 0.19 ± 0.02 | 13.2 | 1f | 0.32 ± 0.13 | 33.4 |
1b | 0.49 ± 0.11 | 19.1 | 1g | 0.59 ± 0.16 | 11.9 |
1c | 0.98 ± 0.24 | 30.0 | 1h | 1.97 ± 0.53 | 17.8 |
1d | 0.085 ± 0.021 | 13.1 | 1i | 4.68 ± 0.85 | 31.6 |
Data are represented as EC50. Values are the means ± SD from three independent experiments.
The plasma half-lives of lixisenatide and 1a–1i were calculated after incubation of peptides in rat plasma over 48 h.