Glucagon Receptor (GCGR) ACTOne Stable Cell Line
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Catalog Number:
CL-01-GCGR
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In Stock
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Price: Please inquire order@eEnzyme.com
Detailed Description
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CL-01-GCGR
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Name
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Glucagon Receptor (GCGR) ACTOneTM Stable Cell Line
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Description
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This cell line is a HEK-293 CNG cell line that expresses a recombinant human GCGR. 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.
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Application
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cAMP dependent human GCGR cell-based assay;
cell-based high-throughput screening of human GCGR agonists/antagonists.
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Size
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1x 106 cells
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Detection
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FlexStation or Microplate reader
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For Downloading
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==>> DATA SHEET ==>> MSDS
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About Human Glucagon Receptor (GCGR) Stable Cell Line
The human glucagon receptor (GCGR) is a Class B (Secretin family) G protein-coupled receptor (GPCR) encoded by the GCGR gene. GCGR is predominantly expressed in the liver and is activated by the peptide hormone glucagon, a key regulator of glucose and energy homeostasis. Upon glucagon binding, GCGR primarily couples to the Gs protein, stimulating adenylyl cyclase, increasing intracellular cAMP levels, and activating protein kinase A (PKA)-mediated signaling pathways. In certain cell types, GCGR signaling may also involve β-arrestin recruitment, ERK1/2 activation, receptor internalization, and additional downstream signaling events.
The eEnzyme Human GCGR ACTOne™ Stable Cell Line stably expresses the human glucagon receptor in HEK293 cells together with the ACTOne™ membrane potential reporter system. This fluorescence-based assay platform provides a sensitive, homogeneous, and high-throughput method for evaluating GCGR activation and inhibition. The cell line is ideally suited for screening glucagon receptor agonists, antagonists, allosteric modulators, and biased ligands, as well as potency determination (EC₅₀/IC₅₀), receptor pharmacology studies, and drug discovery applications.
Applications of the GCGR Stable Cell Line
• High-throughput screening of GCGR agonists, antagonists, and allosteric modulators
• Potency determination (EC₅₀/IC₅₀) of glucagon receptor-targeting compounds
• Characterization of Gs/cAMP-mediated GPCR signaling
• β-arrestin recruitment and biased agonism studies
• Drug discovery for obesity, type 2 diabetes, and metabolic disorders
• Evaluation of GLP-1R/GCGR dual agonists and GIPR/GLP-1R/GCGR triple agonists
• Studies of hepatic glucose production and energy metabolism
• Investigation of glucagon receptor signaling in pancreatic islet biology
• Male reproductive biology and Sertoli cell signaling research
• Diabetes-associated male infertility and reproductive aging studies
Biological Significance of GCGR
GCGR is a central regulator of glucose, lipid, and amino acid metabolism. Activation of GCGR stimulates hepatic glycogenolysis, gluconeogenesis, ketogenesis, and fatty acid oxidation, thereby maintaining blood glucose levels during fasting. In addition to its classical metabolic functions, GCGR signaling contributes to body weight regulation, energy expenditure, pancreatic islet function, and cardiovascular physiology. Abnormal GCGR activity has been implicated in type 2 diabetes mellitus, obesity, metabolic dysfunction-associated steatotic liver disease (MASLD), nonalcoholic steatohepatitis (NASH), cardiovascular disease, and rare glucagon receptor-related disorders, making GCGR an important therapeutic target for next-generation metabolic medicines.
Recent studies have revealed an additional role for GCGR in male reproductive physiology. GCGR is expressed in Sertoli cells, where it regulates glycolytic metabolism and lactate production required to support developing germ cells and maintain blood-testis barrier integrity. Experimental inhibition of GCGR signaling has been shown to improve sperm concentration, motility, and Sertoli cell function in diabetic and aged animal models, suggesting that GCGR may represent a promising therapeutic target for diabetes-associated male infertility and reproductive aging. This emerging biological function further expands the utility of GCGR as a target for both metabolic and reproductive research.
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