The GLP-1 Receptor (GLP-1R) is a class B GPCR regulating glucose homeostasis and energy metabolism. Activated by exenatide, GLP-1R triggers glucose-dependent insulin secretion and glucagon suppression, crucial for glycemic control. It plays a vital role in metabolic disorders like type 2 diabetes and obesity.
GLP-1R signals through cAMP and β-arrestin pathways. The cAMP cascade promotes insulin release and β-cell preservation, while β-arrestin regulates receptor internalization. Dysregulation leads to glucose intolerance, insulin resistance, and dysfunction, making GLP-1R a key diabetes and obesity research target.
Eurofins DiscoverX's cAMP Hunter™ Exenatide Bioassay Kit provides a reliable cell-based assay to measure drug potency and detect neutralizing antibodies. From characterization to QC lot-release, it ensures compound quality and supports drug discovery for metabolic diseases.
In the cAMP Hunter Exenatide Bioassay Kit, CHO-K1 cells overexpressing GLP1R utilize the natural coupling status of the GPCR to Gαs to monitor activation of the receptor. When GLP1R is activated, it stimulates adenylate cyclase, which in turn enables the production of cAMP. The resulting increase in cellular cAMP levels is measured using a homogenous, gain-of-signal competitive immunoassay based on Enzyme Fragment Complementation (EFC) technology.
The signal from the assay is directly proportional to the amount of cellular cAMP in the well, i.e., the higher the GLP1R activation, the greater the cellular cAMP levels, and the larger the signal produced in the assay.
The Exenatide qualification data demonstrates that the cAMP Hunter™ Exenatide Bioassay Kit delivers robust and reproducible performance across all critical assay parameters. Validation studies include intra-plate precision (%CV across eight full-plate dose-response curves), plate uniformity (EC80 and IC80 across each plate), inter-plate variability (three full-plate curves run over three days), slope consistency, relative potency across 50–150%, and parallelism of potency data from two operators. All results have been generated and reviewed by the designated assay developer and qualifier.
Key qualification parameters: