glp-1r

GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).

GLP-1R Agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).

GLP-1R modulator L7-028 is a variant that enhances affinity for GLP-1 and (cAMP) signaling.

GLP-1R modulator C16 is a variable modulator that significantly increases the binding affinity of GLP-4.

GLP-1R agonist 25 (compound 13) is a GLP1-R agonist with an EC50 of 0.167 nM and is utilized in research for Type II diabetes.

Compound 1, also known as GLP-1R agonist 26, is an agonist of the glucagon-like peptide-1 receptor (GLP-1R) with an EC50 of <10 nM.

GLP-1R agonist 27 (compound 21) is a potent and orally active GLP-1R agonist. It enhances the accumulation of cyclic adenosine monophosphate (cAMP), reduces blood glucose levels, and decreases food intake. GLP-1R agonist 27 shows potential for research in obesity and type 2 diabetes mellitus (T2DM).

GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist that enhances insulin secretion and is applicable for research into GLP-1R-related disorders.

GLP-1R agonist 29 (Compound 20) is a GLP-1R agonist that induces hGLP-1R-mediated cAMP stimulation with an EC50 of 0.018 nM. It exhibits favorable pharmacokinetic properties and shows good in vivo exposure, with an AUC0-∞,sc of 77688 ng·h/mL.

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 21 (Compound I-134) is an agonist of the glucagon-like peptide-1 receptor (GLP-1 receptor) with an EC50 of 0.0104 nM.

GLP-1R agonist 22 (Compound I-135) functions as an agonist for the glucagon-like peptide-1 receptor (GLP-1 receptor), with an EC50 of 0.0165 nM.

GLP-1R agonist 20 (Compound I-132) is an agonist of the glucagon-like peptide-1 receptor (GLP-1 receptor), with an EC50 value of 0.0162 nM.

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

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).

GLP-1R agonist 35 (Compound 111-2) is a GLP-1R agonist with an EC50 of 0-10 nM. It is useful for research in diabetes and obesity.

GLP-1R agonist 36 (Compound 53) is a GLP-1R agonist with four isomers, utilized in research related to diabetes and obesity.

GLP-1R agonist 40 (Compound I-1) is an orally active and potent selective GLP-1R agonist with an EC50 of 26.7 pM for cAMP accumulation. It significantly reduces blood glucose levels and can be utilized in research related to type 2 diabetes.

GLP-1R modulator C5 is a small molecule GLP-1R orthosteric modulator that enhances GLP-1 binding to GLP-1R via transmembrane sites and can be used in the study of type II diabetes.

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

GLP-1R agonist 8 is a potent GLP-1R agonist with an EC50 of less than 2 nM.