Agonist potency and efficacy of peptides for the human and rat GLP-2 receptors and selectivity vs. human GLP-1 receptor in cell-based functional assays of cAMP responsive activation
Values are means with 95% confidence interval in parenthesis or means ± S.E.M. of three or more independent assays.
| Peptide | hGLP-2 Receptor | hGLP-1 Receptor | Selectivitya | rGLP-2 Receptor | |||
|---|---|---|---|---|---|---|---|
| EC50 | Emax | EC50 | Emax | GLP-1/GLP-2 | EC50 | Emax | |
| nM | % | nM | % | ratio | nM | % | |
| hGLP-2 | 0.07 (0.06–0.10) | 100 | 517 (403–663) | 71 ± 5 | 7300 | 0.09 (0.06–0.12) | 100 |
| Apraglutide | 0.03 (0.03–0.04) | 95 ± 0 | >1000 | 45 ± 7 | >33,000 | 0.07 (0.05–0.10) | 91 ± 3 |
| Teduglutide | 0.09 (0.07–0.11) | 98 ± 3 | >1000 | 3 ± 0 | >11,000 | 0.08 (0.07–0.09) | 96 ± 1 |
| Glepaglutide | 0.24 (0.17–0.34) | 95 ± 1 | 8.7 (6.6–12) | 97 ± 1 | 36 | 0.42 (0.29–0.63) | 87 ± 2 |
| hGLP-1 | N.D. | 0.02 (0.02–0.03) | 100 | N/A | N.D. | N.D. | |
N/A, not applicable; N.D, not determined.
↵a Ratio of hGLP-1 receptor EC50/hGLP-2 receptor EC50.