GLP Receptor Agonist

Exendin-4-Cys is a cysteine-modified Exendin-4 (HY-13443). Exendin‑4 (Exenatide) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist.

Albiglutide fragment (GLP-1 (7-36) analog) TFA is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment TFA significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies.

Efsubaglutide alfa is a long-acting humanised GLP-1 receptor agonist. Efsubaglutide alfa binds specifically to the GLP-1 receptor, enhancing glucose-dependent insulin secretion, suppressing glucagon release, and promoting β-cell proliferation and increased β-cell mass. Efsubaglutide alfa improves glucose tolerance, increases pancreatic insulin content, and enhances β-cell secretory responses in isolated human islets. Efsubaglutide alfa reduces liver steatosis, lowers NAFLD Activity Scores, improves perisinusoidal collagen features, reduces serum ALT and AST levels, improves fasting glucose and triglyceride levels, and reduces body weight, liver weight and liver-to-body weight ratio. Efsubaglutide alfa can be used for the research of type 2 diabetes. Efsubaglutide alfa can be used for the research of metabolic dysfunction-associated steatohepatitis.

PF-06954522 citrate is an orally active GLP-1R agonist. PF-06954522 citrate can be used for the study of type 2 diabetes mellitus.

Cochinchinenin C is a GLP-1R agonist that binds to the extracellular domain of the receptor via hydrophobic interactions and hydrogen bonds, and promotes glucose-dependent insulin secretion from pancreatic β-cells. Cochinchinenin C also increases intracellular cAMP and ATP levels. At low concentrations, Cochinchinenin C binds to human serum albumin, alters its microenvironment, and induces dominant static fluorescence quenching. Cochinchinenin C shows almost no cytotoxicity to pancreatic β-cells, and exerts a synergistic effect with Loureirin A (HY-N1505) when binding to human serum albumin. Cochinchinenin C has been widely used in studies of type 2 diabetes, Helicobacter pylori infection, thrombotic diseases, and other conditions.

Elecoglipron (AZD5004) is an orally active small-molecule GLP-1R agonist. Its IC₅₀ against human GLP-1R is 2.4 nM. It activates the cAMP signaling pathway in HEK293 cells overexpressing human GLP-1R with a potency of 2.1 nM, and enhances glucose-stimulated insulin secretion in EndoC-βH5 cells with an EC₅₀ of 5.9 nM, with no detectable β-arrestin-2 recruitment or GLP-1R internalization. Elecoglipron can be used in research related to obesity, overweight and type 2 diabetes.

Zantrutide is a glucagon, gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptor agonist. Zantrutide can be used for the study of metabolic diseases.

GLP-1 receptor agonist 22 is an orally active GLP-1 receptor agonist. GLP-1 receptor agonist 22 promotes the accumulation of cAMP. GLP-1 receptor agonist 22 reduces blood glucose levels and inhibits feeding behavior in human glucagon-like peptide-1 receptor knock-in mice. GLP-1 receptor agonist 22 can be used in the research of type 2 diabetes and obesity.

FC382K10W15 is a glucagon analogue and GLP-1R/GCGR agonist. FC382K10W15 can be used in type 2 diabetes research.

Relsipatide (BG128) is a dual gastric inhibitory polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) receptor agonist. Enicepatide can be studied in antidiabetic research.

GLP-1R agonist 18 (example 117) is an agonist for GLP-1R with an EC₅₀ of 0.044 nM.

Birmiglipron is a glucagon-like peptide-1 (GLP-1) receptor agonist. Birmiglipron is applicable for cancer research.

GLP-1R agonist 15 (Compound 101) is a GLP-1 receptor agonist.

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

FC382K10W15 TFA is a glucagon analogue and GLP-1R/GCGR agonist. FC382K10W15 TFA can be used in type 2 diabetes research.

Linvixdutide is a glucagon and glucagon-like peptide 1 receptor (GLP-1R) agonist with anti-obesity effects.

GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research.

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC₅₀ of 0.74 nM. The IC₅₀ for the hERG potassium ion channel is 10.1 μM. GLP-1 receptor agonist 15 can be used for research in the field of diabetes.

GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity.

Retatrutide, Phe22(¹³C₉,¹⁵N) (LY3437943, Phe22(¹³C₉,¹⁵N) TFA is the ¹³C, ¹⁵N-labeled Retatrutide (HY-P3506). Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC₅₀ values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.