Table 1 Phamacokinetics of tirzepatide, mouse GIP and human GIP at the mouse GIP receptor

From: The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets

 

[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)

  1. 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.
  2. *P < 0.05 versus mGIP
  3. **P < 0.05 versus hGIP.
  4. Source data
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