GLP-1R agonist 30 is an orally active, selective GLP-1R agonist with an EC50 of 0.048 nM. It exhibits outstanding selectivity, with EC50 values exceeding 20 µM for GLP-2R, GIPR, and GCPR. GLP-1R agonist 30 significantly enhances cAMP stimulation and reduces hERG inhibition. The compound has good absorption and excellent beta-arrestin pathway selectivity. Additionally, GLP-1R agonist 30 improves glucose tolerance and promotes insulin secretion in B-hGLP1R gene knock-in mice.
Formel:
C33H32F3N5O4
Target-Kategorie:
Glucagon Receptor
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