Table 1.
Phamacokinetics of tirzepatide, mouse GIP and human GIP at the mouse GIP receptor
| [125I]GIP(1-42)OH binding | Gs recruitment | [35S]GTPγS binding | cAMP | ||||
|---|---|---|---|---|---|---|---|
| Peptide | Ki (nM) | EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | EC50 (pM) | Emax (%) |
| mGIP | 0.764 (0.182, 3) | 61.4 (9.8, 9) | 100 (2.46, 9) | 0.181 (2.9, 6) | 98.9 (2.9, 6) | 6.04 (2.0, 3) | 103 (3.9, 3) |
| hGIP | n/a | 152.6 (19.0, 9)* | 101 (2.45, 9) | 0.735 (0.068, 13) | 96.7 (1.3, 13) | 46.0 (16.0, 3) | 102 (4.7, 3) |
| TZP | 24.3 (1.7, 3)* | 153.1 (18.6, 9)* | 72.6 (1.73, 9)* | 5.35 (0.901, 7)*, ** | 88.9 (1.4, 7)*, ** | 363 (68.0, 3)*, ** | 103 (3.5, 3) |
Values are expressed as mean (s.e.m., n). A Student’s t-test was used to compare differences with GIP binding, and a one-way ANOVA with Tukey’s post-hoc test was used for all other comparisons.
*P < 0.05 versus mGIP
**P < 0.05 versus hGIP.