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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.
LSN3318839 is an orally active positive modulator of the glucagon receptor (GCGR). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it valuable in the study of glucose metabolism and diabetes management. It is suitable for research applications focused on metabolic disorders and endocrine signaling pathways.
GLP-1R modulator C5 is an allosteric modulator that enhances the binding of GLP-1 to the GLP-1 receptor (GLP-1R) by interacting with a transmembrane site. It exhibits a half-maximal effective concentration (EC50) of 1.59 ± 0.53 μM. This compound is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into GLP-1R signaling pathways and potential therapeutic applications.
GLP-1R modulator L7-028 is an allosteric modulator that enhances the binding of GLP-1 to the GLP-1 receptor (GLP-1R) through a transmembrane site, with an EC50 of 11.01 ± 2.73 μM. This compound is valuable for investigating GLP-1R signaling pathways and its implications in metabolic disorders. Research applications include studies on glucose homeostasis and potential therapeutic strategies for type 2 diabetes and obesity.
GLP-1R modulator C16 functions as an allosteric modulator by enhancing the binding affinity of GLP-1 to the GLP-1 receptor (GLP-1R) through a transmembrane site, exhibiting an EC50 of 8.43 ± 3.82 μM. This compound is significant for research on glucose homeostasis and diabetes, enabling studies on GLP-1R signaling pathways and therapeutic applications for metabolic disorders. Its modulation potential aids in understanding GLP-1R pharmacology and its implications in drug development.
