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Glucagon receptor antagonists block the receptor through which glucagon raises hepatic glucose output. The glucagon receptor (GCGR) is a class B G protein-coupled receptor (GPCR) expressed mainly in liver and kidney. Expression cloning of the rat receptor in 1993 described its signaling through cyclic adenosine monophosphate (cAMP) and intracellular calcium. Small-molecule antagonists in this list include MK 0893, adomeglivant and PF-06291874, which serve as tools in models of glucose homeostasis and type 2 diabetes. Glucagon (Human, Porcine) is included as the native peptide agonist for receptor activation assays. The set also contains related incretin tools for glucagon-like peptide 1 (GLP-1) research, such as Glucagon-Like Peptide 1 (7-36) Amide and GLP-1R Antagonist 1.
Glucagon (22-29) is a partial agonist of Glucagon (19-29) that targets the glucagon receptor. It is known to specifically inhibit the Ca2+ pump in liver plasma membranes, functioning independently of adenylate cyclase activation. This compound is useful in research applications focused on metabolic regulation and signaling pathways related to glucagon action in hepatocytes.
