GLP1R (glucagon-like peptide-1 receptor) is a class B GPCR that plays a central role in metabolic regulation by mediating cAMP signaling in response to GLP-1 and related agonists. It is an important target in metabolic diseases, especially type 2 diabetes and obesity, where GLP-1-based therapies have become highly effective treatment options and continue to drive drug discovery interest.
The cAMP Hunter™ Human GLP-1 (GLP1R) Gs Stable Cell Line Assay (CHO-K1) enables quantitative measurement of receptor activation through intracellular cAMP detection, supporting potency, efficacy, and rank-order profiling of small molecules and biologics. Its stable CHO-K1 format, cryopreserved cells, and chemiluminescent EFC readout make it a practical and robust tool for GPCR pharmacology and mechanism-of-action studies.
In the cAMP Hunter Human GLP 1 (GLP1R) Gs Stable Cell Line Assay (CHO K1), CHO K1 cells overexpressing human GLP 1R leverage the receptor’s natural Gαs coupling to monitor activation. When stimulated by GLP 1 or related agonists, GLP1R activates adenylyl cyclase, which catalyzes 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, such that greater GLP 1R activation produces higher cAMP concentrations and larger assay signals.
The cAMP Hunter™ Human GLP-1 (GLP1R) Gs Stable Cell Line Assay (CHO-K1, cat. no. 795-0062C2) offers dual-protocol flexibility: a traditional adherent mode for overnight cell attachment and standard workflows, and a streamlined suspension mode for same-day results in ~3 hours with reduced hands-on time. Both deliver equivalent potency (e.g., Exendin-4 EC50), high signal-to-background ratios, and seamless EFC-based cAMP detection, validated specifically for this GLP1R line to support HTS, automation, or routine screening.
The following graphs show typical results obtained with the cAMP HitHunter kit using two different workflows, demonstrating robust performance regardless of the workflow chosen.