Biological Background

The Gastric Inhibitory Polypeptide Receptor (GIPR) is a GPCR involved in glucose homeostasis and lipid metabolism. Activated by GIP, it enhances insulin secretion and regulates lipids. Dysregulation can lead to metabolic disorders like type 2 diabetes and obesity.

GIPR neurons in the brain influence long-term food intake and body weight. Activation can reduce both without aversive effects, making GIPR a target for obesity treatment. GIPR signals through Gs protein, increasing intracellular cAMP, a key pathway in glucose regulation, lipid metabolism, and obesity.

Eurofins DiscoverX's cAMP Hunter™ GIPR Gs cell line (HEK293) provides a robust tool for studying GIPR-targeting drug candidates. This engineered cell line enables accurate ligand-based activation assessment and supports drug discovery for metabolic disorders and obesity.

Product Highlights
  • Validated GIPR stable cell line
  • Detects intracellular cAMP levels as a response to GIPR activation
  • Wild-type GIPR
  • Suitable for GIPR drug discovery on small and large molecules
  • Designed to be used with HitHunter cAMP Assay Detection kit

cAMP GIPR Assay Principle

The cAMP Hunter™ GIPR Gs Cell Line overexpresses GIPR in a HEK293 cell background. When used in conjunction with the HitHunter® cAMP Assay Detection Kit, it utilizes the natural coupling status of GIPR to Gαs to monitor receptor activation. When GIPR is activated by GIP, a reference agonist for this receptor, it stimulates adenylate cyclase, which in turn enables the production of cAMP. The resulting increase in cellular cAMP levels is measured using a homogeneous, 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 GIPR activation, the greater the cellular cAMP levels, and the larger the signal produced in the assay.

cAMP CALCR Gs Cell line Assay Principle