GLP-1R agonist 3

GLP-1R agonist 3 is a potent imidazole derivative and GLP-1R agonist with demonstrated research potential in diabetes. [Thickened]

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 β-arrestin pathway selectivity. Additionally, GLP-1R agonist 30 improves glucose tolerance and promotes insulin secretion in B-hGLP1R gene knock-in mice.

Exendin-4 (3-39) is a truncated peptide variant of Exendin-4, missing the initial two amino acids, and serves as a potent agonist for the Glucagon-like peptide-1 receptor (GLP-1r). This compound, along with Exendin-4, is utilized in the study of diabetes and hypothalamic-pituitary-adrenal (HPA) axis disorders [1] [2].

Oxyntomodulin (swine), a peptide hormone secreted from the gastrointestinal tract after meals, serves as a dual agonist for the GLP-1 receptor (GLP-1R) and glucagon receptor (GCGR). It plays a critical role in appetite suppression and the reduction of food intake [1] [2] [3].