GLP Receptor Agonist

GLP-1R agonist 34 (Compound 1) is an orally active small molecule glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 34 promotes insulin secretion, inhibits glucagon release, and delays gastric emptying, thereby effectively lowering blood glucose levels. GLP-1R agonist 34 is promising for research of metabolic diseases, including type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

Bilpatide (RAY1225) is a dual agonist of glucagon-like peptide-1 receptor (GLP-1R) and glucose-dependent insulinotropic polypeptide receptor (GIPR). Bilpatide is applicable to research related to obesity and diabetes.

GLP-1R/GIPR agonist-2 is a GIPR agonist. GLP-1R/GIPR agonist-2 potentiates GIP(1-42)-induced intracellular cAMP production in cells expressing human GIPR. GLP-1R/GIPR agonist-2 can be used for the research of type II diabetes mellitus.

(Asp28)-Exenatide is a degradation product of exenatide (HY-13443). (Asp28)-Exenatide can be used as a GLP-1R agonist.

GLP-1R agonist 44 is a glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R agonist 44 can be used for the research of diseases related to GLP-1R, such as type 2 diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, nephropathy, gout, hematuria, cardiovascular disease.

Vensemaglutide is the agonist for glucagon-like peptide 1 (GLP-1) receptor. Vensemaglutide can be used in research of diabetes or other metabolic disorders.

Taspoglutide (R1583) acetate is an agonist of the glucagon-like peptide 1 receptor (GLP-1R) with an K_i value of 1.1 nM. Taspoglutide acetate induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC₅₀ = 0.06 nM). Taspoglutide acetate decreases blood levels of glucose and increases blood levels of insulin in a glucose tolerance test in Zucker diabetic obese rats. Taspoglutide acetate reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model.

GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist. GLP-1R agonist 28 can increase insulin secretion and can be used in the research of GLP-1R-related diseases.

Anvoglutide is a glucagon-like peptide 1 (GLP-1) receptor agonist with antidiabetic and obesity effects.

Tirzepatide sodium (LY3298176 sodium) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Tirzepatide sodium exerts anti-apoptotic and pro-differentiation effects via the pAkt/CREB/BDNF cascade and miRNA in neurons; in the heart, it promotes BCAA catabolism and inhibits the mTOR pathway by mediating the dephosphorylation of BCKDHA; meanwhile, it effectively reduces insulin and leptin levels and suppresses inflammatory responses at the systemic level. Tirzepatide sodium can be used for research on myocardial infarction, colon cancer, diabetes, diabetic cognitive impairment, neurodegeneration, diabetes-related neuropathy, and obesity.

GLP-1R modulator-1 (Compound 384) is an orally active, potent selective glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R modulator-1 activates G-protein coupled signaling, elevates intracellular cAMP levels, promotes insulin secretion, delays gastric emptying and suppresses appetite. GLP-1R modulator-1 is promising for research of type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

Liraglutide acetate is the acetate form of Liraglutide (HY-P0014), a glucagon-like peptide-1 (GLP-1) receptor agonist studied in type 2 diabetes.

d-GLP-2 E33A is an agonist for the glucagon-like peptide 2 receptor (GLP-2R) with an EC₅₀ of 414 nM. d-GLP-2 E33A can activate GLP-2R and increase the phosphorylation of AKT, but has no stimulative effect on GLP-1R. d-GLP-2 E33A can be used in the study of diseases such as intestinal malabsorption and inflammatory bowel diseases.

UTG-4 is a GLP-1R, GIPR, and GCGR agonist with EC₅₀ values of 126.3 pM, 29.2 pM, and 250.2 pM, respectively. UTG-4 binds to HSA (K_d = 14.6 μM). UTG-4 effectively alleviates endothelial-mesenchymal transition. UTG-4 promotes weight loss, inhibits food intake, improves glucose tolerance, and has a significant anti-atherosclerotic effect.

GLP-1R-agonist-43 (Compound A) is an orally active GLP-1R agonist with an EC₅₀ of 2.68 nM. GLP-1R-agonist-43 can be used in the research of non-insulin-dependent diabetes mellitus (type 2 diabetes) and obesity.

GLP-1R agonist 36 (Compound 53) is a GLP-1R agonist with a total of four isomers. GLP-1R agonist 36 can be used for the studies of diabetes and obesity.

GLP-1R agonist 42 is an agonist for glucagon-like peptide-1 receptor (GLP-1 receptor), with EC₅₀ of 0.0122 nM.

DA5-CH (KP405) is a blood-brain barrier-permeable GLP-1/GIP receptor agonist. DA5-CH activates GLP-1 and GIP receptors, inhibits the NF-κB inflammatory pathway, reduces α-synuclein (α-synuclein) levels, restores the expression of tyrosine hydroxylase and neurotrophic factors, improves motor function, decreases amyloid plaques and phosphorylated tau protein levels in the hippocampus, restores synaptic plasticity, regulates the PI3K/AKT/GSK3β and CREB signaling pathways, and alleviates mitochondrial stress. DA5-CH can be used for research on Parkinson's disease and Alzheimer's disease.

TC2 is an efficient GIPR-preferring monomeric quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.47, 2.1, 30, and 55 nM respectively. TC2 exhibits a significant GLP-1R preference, with a significant reduction in β-inhibitory protein 2 (βArr2) recruitment, while maintaining a strong cAMP signal. TC2 can be used for research on obesity and diabetes.

Erzemdutide is a glucagon and glucagon-like peptide 1 (GLP-1) receptor agonist. Erzemdutide can be used for the study of obesity.