The GIP receptor (GIPR), a class A GPCR integral to incretin signaling, enhances insulin release and fat metabolism, positioning it as a vital target for obesity, type 2 diabetes, and cardiometabolic therapies.
This cAMP Hunter™ Human GIPR Gs Stable Cell Line Assay (HEK293, cat. no. 795-1186C1) features HEK293 cells engineered for sensitive detection of GIP-stimulated cAMP via Gαs-mediated adenylyl cyclase activation. Its homogeneous EFC chemiluminescent platform facilitates agonist/antagonist potency assessment, efficacy evaluation, and comparative profiling in GIPR drug discovery programs.
In the cAMP Hunter Human GIPR Gs Stable Cell Line Assay (HEK 293), HEK 293 cells overexpressing human GIPR leverage the receptor’s natural Gαs coupling to monitor activation. When stimulated by GIP or related agonists, GIPR 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 GIPR activation produces higher cAMP concentrations and larger assay signals.
The cAMP Hunter™ Human GIPR Gs Stable Cell Line Assay (HEK293, cat. no. 795-1186C1) provides versatile dual-format options: adherent mode for conventional overnight plating and established lab routines, plus suspension mode enabling complete same-day execution (~3 hours) with fewer manual steps. Each protocol maintains identical GIP potency (e.g., EC50 values), excellent signal windows, and reliable EFC chemiluminescent cAMP readout, fully validated for this cAMP HEK293 GIPR cell line to power high-throughput screening, automated systems, or daily pharmacology assays.
Suspension mode eliminates overnight plating by seeding cells directly into cAMP Cell Assay Buffer, enabling faster turnaround without compromising data quality.
The following graphs show typical results obtained on cAMP Hunter GIPR Gs Cell Line (HEK 293) with the cAMP HitHunter kit using two different workflows, demonstrating robust performance regardless of the workflow chosen.