Glucagon-Like Peptide 1 Receptor (GLP1R) ACTOne Stable Cell Line

Catalog Number:
CL-01-GLP1R
In Stock
Price: Please inquire order@eEnzyme.com
Detailed Description

CL-01-GLP1R

Name

Glucagon-Like Peptide 1 Receptor (GLP1R) ACTOneTM Stable Cell Line

Description

This cell line is a HEK-293 CNG cell line that expresses a recombinant human GLP1R. HEK-293 CNG-Slcla3 cells express a modified CNG (Cyclic Nucleotide Gated) channel that opens in response to elevated intracellular cAMP levels and consequently result in ion flux and cell membrane depolarization. The assay allows both end-point and kinetic measurement of intracellular cAMP changes with a FLIPR or a fluorescence microplate reader.

Application

cAMP dependent human GLP1R cell-based assay;

cell-based high-throughput screening of human GLP1R agonists/antagonists.

Size

1x 106 cells

Detection

FlexStation or Microplate reader

For Downloading

==>> DATA SHEET      ==>> MSDS



Synonym: GLP-1R, Glucagon-Like Peptide 1 Receptor, GLP-1 Receptor, GLP-1-R, Seven Transmembrane Helix Receptor, GLP1 Receptor, GLP-1

About Human Glucagon-Like Peptide-1 Receptor (GLP1R) Stable Cell Line

Glucagon-Like Peptide-1 Receptor (GLP1R) is a Class B G protein-coupled receptor (GPCR) that serves as the primary receptor for glucagon-like peptide-1 (GLP-1), an incretin hormone secreted by intestinal L-cells in response to nutrient intake. GLP1R is predominantly expressed in pancreatic β-cells but is also found in the gastrointestinal tract, brain, heart, kidney, and other tissues. Upon activation by GLP-1, GLP1R primarily couples to Gs proteins, stimulating adenylate cyclase activity and increasing intracellular cAMP levels. This signaling pathway enhances glucose-dependent insulin secretion, suppresses glucagon release, delays gastric emptying, and promotes satiety, making GLP1R a critical regulator of glucose homeostasis and energy balance.

GLP1R has become one of the most important therapeutic targets in modern metabolic medicine. The remarkable clinical success of GLP-1 receptor agonists, including semaglutide, liraglutide, dulaglutide, and tirzepatide-based combination therapies, has demonstrated the significant potential of GLP1R-targeted therapeutics for the treatment of type 2 diabetes, obesity, cardiovascular disease, and metabolic syndrome. As a result, GLP1R remains a major focus of pharmaceutical research, receptor pharmacology, and next-generation drug discovery programs.

eEnzyme's Human GLP1R Stable Cell Line provides a reliable and reproducible cellular platform for investigating GLP1R-mediated signaling pathways and evaluating receptor-targeted therapeutics. The cell line enables quantitative assessment of agonists, antagonists, peptide analogs, biosimilars, and allosteric modulators through cAMP assays, reporter gene assays, and other GPCR functional screening platforms. Researchers can utilize this stable cell line for receptor characterization, potency determination, lead optimization, biosimilar comparability studies, and high-throughput screening applications supporting diabetes and obesity drug discovery.

Applications of the GLP1R Stable Cell Line

• GLP1R receptor pharmacology studies
• GLP-1 analog and agonist screening
• Type 2 diabetes drug discovery
• Obesity and weight management research
• cAMP and GPCR signaling assays
• Biosimilar potency and comparability testing
• Metabolic disease therapeutic development
• High-throughput screening applications

Biological Significance of GLP1R

GLP1R is a central regulator of glucose metabolism and energy homeostasis. Activation of GLP1R enhances glucose-dependent insulin secretion while suppressing glucagon release, resulting in improved glycemic control with a low risk of hypoglycemia. In addition, GLP1R signaling slows gastric emptying, reduces appetite, promotes weight loss, and exerts beneficial effects on cardiovascular and metabolic health. Because of these diverse physiological actions, GLP1R-targeted therapies have transformed the treatment landscape for obesity and type 2 diabetes. Ongoing research continues to explore the role of GLP1R in cardiovascular protection, neuroprotection, liver disease, and combination incretin therapies. As one of the most clinically successful GPCR targets, GLP1R remains a cornerstone of metabolic disease research and pharmaceutical innovation. The GLP1R Stable Cell Line provides a valuable tool for studying incretin receptor biology and accelerating the development of next-generation therapeutics targeting diabetes, obesity, and related metabolic disorders.

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