- Cat. No.
- A13781
BETP
BETP is a selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
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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.
BETP is a selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
VU0453379 is a CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) with an EC50 of 1.3 μM.
NNC0640 is a negative allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R).
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.
GPCR modulator-1 is a negative allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound demonstrates key biological activity by modulating receptor signaling, making it valuable for investigating the role of GLP-1R in type 2 diabetes research. GPCR modulator-1 can facilitate studies aimed at understanding metabolic processes and potential therapeutic interventions for diabetes-related complications.
(S,R)-LSN3318839 is a stereoisomer of LSN3318839, functioning as a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it a valuable reagent for research into diabetes and metabolic disorders. Its oral bioactivity positions it as a promising candidate for studies focused on glucose homeostasis andtherapeutic interventions.
V-0219 is an orally active positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). This compound enhances GLP-1R signaling, making it a valuable tool for studying therapeutic strategies in obesity-associated diabetes and related metabolic disorders. Its mechanism of action offers potential insights into the modulation of glucose homeostasis and appetite regulation.
LSN3160440 is an allosteric modulator of the GLP-1 receptor (GLP-1R) that enhances protein-protein interactions, effectively functioning as a molecular glue. By stabilizing the binding of inactive GLP-1 (9-36) NH2 to GLP-1R, it facilitates receptor activation and downstream signaling. This compound is valuable in studying metabolic disorders and diabetes-related research, providing insights into GLP-1R modulation and its therapeutic potential.
V-0219 hydrochloride is a positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). This compound has demonstrated oral bioactivity and is pertinent in the study of obesity-associated diabetes. Its ability to enhance GLP-1R signaling makes it a valuable tool for research into metabolic disorders and therapeutic interventions targeting glucose homeostasis.
(S)-V-0219 is a selective positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). It induces calcium flux in HEK293 cells expressing human GLP-1R, enhancing receptor activity. In vivo studies demonstrate that (S)-V-0219 is orally bioavailable, effectively reducing hyperglycemia in murine models while also suppressing feeding behavior in fasting conditions. This compound presents valuable applications in diabetes research and appetite regulation studies.
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(R)-V-0219 is a positive allosteric modulator of the GLP-1 receptor (GLP-1R), functioning through enhanced receptor activation. It promotes calcium flux in human embryonic kidney (HEK) cells expressing hGLP-1R, indicating its role in metabolic regulation. This compound is particularly relevant for research focused on type 2 diabetes and obesity, allowing scientists to explore the therapeutic potentials of GLP-1R modulation.
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GLP-1R agonist 39 is a potent positive allosteric modulator of the GLP-1 receptor. This compound enhances the activity of the GLP-1 receptor, making it valuable for studies related to obesity and type 2 diabetes. Its application in research enables the exploration of therapeutic strategies aimed at metabolic disorders.