cAMP Hunter™ Human GLP-1 (GLP1R) Gs Stable Cell Line Assay (HEK 293)
The cAMP Hunter™ Human GLP-1 (GLP1R) Gs Stable Cell Line Assay (HEK 293) contains a stable clonal cell line used to measure GLP1R (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 #: 795-1185C1
Size: Kit
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Overview
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Biological Background
GLP1R is a class B GPCR that plays a key role in metabolic signaling, and it remains a major target in obesity and type 2 diabetes drug discovery.
In this cAMP Hunter Human GLP-1 (GLP1R) Gs Stable Cell Line Assay (HEK 293), the receptor is expressed in a HEK293 background to provide a robust functional system for measuring cAMP responses after ligand stimulation. Because GLP1R is naturally coupled to Gαs, receptor activation leads to an increase in intracellular cAMP that can be quantified with a homogeneous EFC-based readout.
This assay supports potency, efficacy, and rank-order profiling of GLP1R ligands in a format designed for drug discovery and development workflows.
Product Highlights
- HEK293 cell background for functional GLP1R cAMP signaling studies.
- Measures ligand-induced receptor activation through intracellular cAMP accumulation.
- Uses a homogeneous, gain-of-signal EFC detection format for simple assay execution.
- Supports potency, efficacy, and rank-order profiling of GLP1R ligands.
- Optimized for GPCR drug discovery and metabolic disease research.
cAMP Hunter Human GLP1R Gs Stable Cell Line Assay (HEK 293) Assay Principle
In the cAMP Hunter Human GLP 1 (GLP1R) Gs Stable Cell Line Assay (HEK 293), HEK 293 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.
cAMP Hunter™ GLP1R (HEK 293) Dual Protocols: Suspension & Adherent
The cAMP Hunter™ GLP1R HEK293 assay (# 795-1185C1) supports both adherent (overnight plating for established workflows) and suspension (3-hour same-day execution with minimal handling) formats, maintaining consistent pharmacology like Exendin-4 EC50 values across conditions.
Suspension mode bypasses overnight culture by direct buffer seeding, ideal for automation or rapid iteration.
Typical Results: Suspension vs. Adherent
The following graphs show typical results obtained on cAMP GLP1R Gs Cell Line (HEK 293) with the cAMP HitHunter kit using two different workflows, demonstrating robust performance regardless of the workflow chosen.
Typical results obtained on cAMP Hunter GLP1R Gs Cell Line (HEK 293) (#795-1185C1). Exendin-4 dose-response curves generated using cAMP HitHunter kit in adherent mode (A.) and suspension mode (B.). Note: the number of cells in suspension mode was decreased from 10,000 cells per well to 5,000 cells per well.