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GLP-1 receptor agonists and modulators act on the receptor for glucagon-like peptide 1 (GLP-1), an incretin hormone. Intestinal L cells release GLP-1 after a meal, and the hormone enhances glucose-dependent insulin secretion from pancreatic beta cells. The receptor, a class B G protein-coupled receptor, was cloned from beta cells by expression cloning in 1992. Peptide agonists in this category include liraglutide and lixisenatide, while tirzepatide also acts at the glucose-dependent insulinotropic polypeptide (GIP) receptor. BETP is a small-molecule ligand that binds the GLP-1 receptor outside the peptide site. The set also includes dipeptidyl peptidase 4 (DPP-4) inhibitors such as linagliptin, which slow the breakdown of endogenous GLP-1.
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
Synonyms: Avexitide
Avexitide (Exendin (9-39)) is a specific and competitive GLP-1 receptor antagonist.
GLP-1(9-36)amide is a potent antagonist of the glucagon-like peptide-1 (GLP-1) receptor, generated from the enzymatic action of dipeptidyl peptidase-4 (DPP-4) on GLP-1(7-36)amide. This peptide plays a crucial role in glucose metabolism and insulin signaling and is utilized in research aimed at understanding metabolic disorders and the role of GLP-1 in obesity and diabetic conditions. The study of GLP-1(9-36)amide can provide insights into receptor regulation and potential therapeutic strategies for GLP-1 related pathologies.
Exendin (5-39) is a selective glucagon-like peptide 1 (GLP-1) receptor antagonist. This compound has been shown to effectively ameliorate memory impairment in β-amyloid protein-treated rodents, making it a valuable tool for studying cognitive decline and neurodegenerative diseases. Its ability to modulate GLP-1 signaling pathways positions Exendin (5-39) as a useful reagent in research focused on metabolic disorders and brain function.
Synonyms: Avexitide acetate
Exendin(9-39) amide acetate is a potent glucagon-like peptide-1 (GLP-1) antagonist that selectively competes with endogenous GLP-1 for the GLP-1 receptor (GLP-1R). By inhibiting GLP-1 signaling, it counteracts the physiological effects associated with elevated GLP-1 levels. This reagent is particularly valuable for research into postbariatric hypoglycemia (PBH) and other metabolic disorders where GLP-1 modulation is critical.
Synonyms: MBX 1416
Imapextide is a glucagon-like peptide-1 (GLP-1) receptor antagonist that plays a critical role in the study of hypoglycemia. By inhibiting GLP-1 activity, Imapextide provides insights into glucose homeostasis and insulin secretion regulation. It is a valuable tool for researchers investigating metabolic disorders and the physiological effects of GLP-1 signaling.
GIPR Antagonist 2 is a potent antagonist of the GIP receptor, which plays a crucial role in glucose metabolism and energy homeostasis. This compound demonstrates significant potential for research applications related to obesity and type 2 diabetes. Its ability to inhibit GIPR signaling provides a valuable tool for investigating the underlying mechanisms of metabolic disorders and evaluating therapeutic strategies.
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