GLP Receptor Antagonist

Exendin (9-39) amide (Avexitide) is a competitive GLP-1R antagonist. Exendin (9-39) amide blocks the Semaglutide (HY-114118)-induced increase in insulin secretion and also attenuates the hypoglycemic effect of Semaglutide. Exendin (9-39) amide abolishes the islet-protective effect of Liraglutide. Exendin (9-39) amide can be used in research on type 2 diabetes and type 1 diabetes.

Exendin (9-39) amide acetate (Avexitide acetate) is a competitive GLP-1R antagonist. Exendin (9-39) amide acetate blocks the Semaglutide (HY-114118)-induced increase in insulin secretion and also attenuates the hypoglycemic effect of Semaglutide. Exendin (9-39) amide acetate abolishes the islet-protective effect of Liraglutide. Exendin (9-39) amide acetate can be used in research on type 2 diabetes and type 1 diabetes.

Pemvidutide (ALT-801) TFA is a GLP-1R/GCGR dual agonist, shows striking reductions in body weight, liver fat and serum lipids. Pemvidutide TFA can be used in non-alcoholic steatohepatitis (NASH) and obesity research.

Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn.

Imapextide is a glucagon-like peptide-1 (GLP-1) receptor antagonist that can be used in hypoglycemia research.

SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency.

DS79932728 is an orally active inhibitor for G9a and GLP with IC₅₀ of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models.

GLP2 (rat) (11-33) is a glucagon-like peptide-2 receptor (GLP-2 receptor) antagonist. GLP2 (rat) (11-33) has weak intrinsic agonistic activity on human GLP-2R; it can synergistically enhance the activity of agonistic allosteric regulators on human, cynomolgus monkey, dog and Syrian hamster GLP-2R, but reduces this activity on rat GLP-2R. GLP2 (rat) (11-33) can be used for GLP-2R related research.

GLP-1R agonist 35 (Compound 111-2) is a GLP-1R agonist with an EC₅₀ of 0-10 nM. GLP-1R agonist 36 can be used for the studies of diabetes and obesity.