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.

GLP-1R agonist 32 (Compound 111) is an orally active and potent GLP-1R agonist with an EC50 value of 0.017 nM. It stimulates the production of cyclic adenosine monophosphate (cAMP) by activating GLP-1R, which enhances insulin secretion, suppresses glucagon release, and delays gastric emptying to regulate blood glucose levels. GLP-1R agonist 32 shows potential for research in type 2 diabetes, obesity, and related metabolic disorders.

GLP-1R agonist 31 (Compound 1) is an amorphous glucagon-like peptide-1 receptor (GLP-1R) agonist.

GLP-1R agonist 33 (Compound 224) is a GLP-1 receptor agonist with potential applications in research related to diabetes, obesity, and non-alcoholic fatty liver disease (NAFLD).

GLP-1R agonist 34 (Compound 1) is an orally active small molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R). It enhances insulin secretion, suppresses glucagon release, and slows gastric emptying, thereby effectively reducing blood glucose levels. GLP-1R agonist 34 holds potential for research into metabolic disorders such as type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

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].