cAMP Hunter™ Human Glucagon (GCGR) Gs Stable Cell Line Assay (CHO-K1)
The cAMP Hunter™ Human Glucagon (GCGR) Gs Stable Cell Line Assay (CHO-K1) contains a stable clonal cell line used to measure GCGR (GPCR) activity via increased levels of intracellular cAMP. This is a complete kit that includes the cell line vials, all required culture reagents for maintaining the cells in continuous culture, and detection reagents for running the assay.
Catalog #: 795-0042C2
Size: Kit
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Biological Background
GCGR (glucagon receptor), a class B GPCR that regulates hepatic gluconeogenesis, glycogenolysis, and energy balance, is increasingly targeted for type 2 diabetes, obesity, and NASH due to its role in countering incretin therapies.
This cAMP Hunter™ Human Glucagon (GCGR) Gs Stable Cell Line Assay (CHO-K1, cat. no. 795-0042C2) harnesses CHO-K1 cells for accurate measurement of glucagon-elicited cAMP elevation through Gαs coupling and adenylyl cyclase activation. Featuring a homogeneous EFC chemiluminescent readout, it excels in agonist/antagonist potency, efficacy profiling, and rank-ordering to advance GCGR modulators and multi-target metabolic candidates.
Product Highlights
- CHO-K1 cells optimized for wild-type human GCGR Gs-mediated cAMP assays
- Sensitive detection of glucagon effects on intracellular cAMP signaling.
- Homogeneous EFC system for straightforward, high-throughput GPCR analysis.
- Facilitates potency, efficacy, and ligand ranking for glucagon therapeutics.
- Suited for diabetes/obesity research and glucagon pathway modulation.
cAMP Hunter Human GCGR Gs Stable Cell Line Assay (CHO-K1) Assay Principle
In the cAMP Hunter Human GCGR Gs Stable Cell Line Assay (CHO K1), CHO K1 cells overexpressing human GCGR leverage the receptor’s natural Gαs coupling to monitor activation. When stimulated by Glucagon or related agonists, GCGR 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 GCGR activation produces higher cAMP concentrations and larger assay signals.
cAMP Hunter™ GCGR Dual Protocols: Suspension & Adherent
The cAMP Hunter™ Human Glucagon (GCGR) Gs Stable Cell Line Assay (CHO-K1, cat. no. 795-0042C2) 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., glucagon EC50), high signal-to-background ratios, and seamless EFC-based cAMP detection, validated specifically for this GCGR line to support HTS, automation, or routine screening.
Suspension mode eliminates overnight plating by seeding cells directly into cAMP Cell Assay Buffer, enabling faster turnaround without compromising data quality.
Typical Results: Suspension vs. Adherent
The following graphs show typical results obtained on cAMP GCGR Gs Cell line with the cAMP HitHunter kit using two different workflows, demonstrating robust performance regardless of the workflow chosen.
Typical results obtained on cAMP Hunter GCGR Gs Cell Line (CHO-K1) (#795-0042C2). Glucagon dose-response curves generated using cAMP HitHunter kit in adherent mode (A.) and suspension mode (B.).