Metabolic features of reference apelins and homologue-substituted apelins. Experiments were done in triplicates. Errors represent standard error of the mean (S.E.M.).
| Analogue | t1/2 human NEP (h) | t1/2 human plasma (h) | t1/2 mice plasma (h) | Plasma protein binding efficacy (%) | |
|---|---|---|---|---|---|
| 1 | Apelin13A2 | 10.31 ± 0.01 | 0.81 ± 0.20 | ||
| 2 | NMeLeu13A2 | 40.27 ± 0.01 | 3.54 ± 0.12 | ||
| 3 | hArg13A2 | 19.01 ± 0.01 | 1.31 ± 0.42 | ||
| 4 | Cha13A2 | 22.07 ± 0.01 | 1.77 ± 0.34 | ||
| 5 | hArgCha13A2 | 21.91 ± 0.02 | 2.58 ± 0.19 | ||
| 6 | Apelin17A2 | 10.95 ± 0.03 | 0.90 ± 0.17 | 57 ± 10 | |
| 7 | NMeLeu17A2 | >48 | 8.29 ± 0.21 | 0.99 ± 0.11 | 55 ± 10 |
| 8 | hArg17A2 | 40.59 ± 0.01 | 3.06 ± 0.04 | ||
| 9 | Cha17A2 | 47.03 ± 0.01 | 4.34 ± 0.03 | ||
| 10 | hArgCha17A2 | 46.39 ± 0.01 | 6.28 ± 0.02 | 0.52 ± 0.12 | 65 ± 9 |
| 11 | NMeCha17A2 | 2.90 ± 0.03 | 0.44 ± 0.07 | 68 ± 8 | |
| 12 | hArgNMeCha17A2 | 3.41 ± 0.05 | 0.36 ± 0.25 | 69 ± 8 | |
| 13 | hArgNMeLeu17A2 | 5.63 ± 0.08 | 0.38 ± 0.21 |