Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).
[Des-His1,Glu9]-Glucagon amide TFA is a potent peptide antagonist targeting the glucagon receptor, featuring a pA2 value of 7.2. It holds potential utility in diabetes pathogenesis research[1].
Glucagon receptor antagonist I is a competitive antagonist of the glucagon receptor (GCGR; IC50 = 181 nM). It blocks glucagon-induced glycogenolysis in primary human hepatocytes and isolated liver. Glucagon receptor antagonist I, at 50 mg/kg, reduces the increase in glucose levels observed after intraperitoneal administration of glucagon in humanized mice. Glucagon receptor antagonist inactive control does not prevent glucagon-mediated actions.
Glucagon, a peptide hormone derived from proglucagon in pancreatic α cells, regulates glucose metabolism. It stimulates glucose production in rat hepatocytes ex vivo and enhances glucose output from perfused rat livers through elevated gluconeogenesis and glycogenolysis, while reducing glycolysis, and raises plasma glucose levels in rats. Glucagon secretion decreases following food intake in healthy rats and humans, yet remains unchanged or increases in individuals with type 2 diabetes.
Glucagon-like peptide 1 (1-37), human (TFA), is a highly potent agonist of the GLP-1 receptor and is a pancreatic hormone synthesized through post-translational processing of proglucagon.
Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized through post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it has no effect on food intake in rats.
Glucagon-like peptide 2 (GLP-2) is a recently identified intestinal epithelium-specific growth factor that has been shown to reduce the severity of inflammatory disorders of the intestine in rodent models. Currently Glucagon-Like Peptide 2 is used as a po