Biological Background

The Glucagon-Like Peptide-1 Receptor (GLP-1R) is a class B GPCR expressed in pancreatic β-cells, brain, and gastrointestinal tract. Activated by GLP-1 receptor agonists, GLP-1R couples to Gαs proteins, stimulating adenylyl cyclase and increasing cAMP. This triggers glucose-dependent insulin secretion, glucagon suppression, and β-cell preservation.

GLP-1R signals through cAMP-PKA and β-arrestin pathways. The Gαs-cAMP cascade enhances insulin exocytosis during hyperglycemia while preserving β-cell function. β-arrestin signaling contributes to desensitization. Dysregulation is implicated in diabetes, obesity, and metabolic syndrome.

Eurofins DiscoverX's cAMP Hunter™ GLP-1 RA Bioassay Kit provides a functional cell-based assay to assess agonist potency and detect neutralizing antibodies. This kit supports drug development from characterization through commercial release, stability testing.

Product Highlights
  • Functional cell-based assay with ready-to-use cryopreserved CHO-K1 cells overexpressing human GLP-1R
  • Robust EFC technology provides highly sensitive, homogeneous cAMP detection with chemiluminescent readout
  • Two kit formats: complete with positive control agonist (exendin-4) or without control ligand
  • Optimized for 96-well format with adaptability to 384-well plate layouts for flexibility
  • Complete materials included: cells, plating reagent, dilution buffer, detection reagents, and assay plates

cAMP Hunter GLP1-RA Assay Principle

In the cAMP Hunter™ GLP-1 RA Bioassay Kit, CHO-K1 cells overexpressing human GLP-1R utilize the receptor's natural Gαs coupling to monitor activation. When stimulated by GLP-1 receptor agonists such as exendin-4, the receptor activates adenylyl cyclase, catalyzing ATP conversion to 3′-5′ cyclic adenosine monophosphate (cAMP). The resulting increase in intracellular cAMP is quantified using a homogeneous, gain-of-signal competitive immunoassay based on Enzyme Fragment Complementation (EFC) technology.

Signal intensity correlates directly with cellular cAMP levels, greater GLP-1R activation produces higher cAMP concentrations and larger assay signals.

cAMP Hunter GLP1-RA assay principle