Human Gastric Inhibitory Polypeptide Receptor Reporter Assay System

This assay utilizes proprietary human cells that have been engineered to provide constitutive expression of Human Gastric Inhibitory Polypeptide Receptor (GIPR). Gastric Inhibitory Polypeptide (GIP), the primary activator of GIPR, is a gut-derived hormone that is secreted from the enteroendocrine K cells of the small intestine in response to nutrient intake. GIP, along with a related hormone, glucagon-like peptide-1 (GLP-1), constitute the incretin hormones that regulate glucose tolerance / levels by stimulating insulin release from pancreatic β-cells. GIPR belongs to the class B1 G protein-coupled receptor (GPCR) superfamily and signals through Gα_s/adenylyl cyclase activation, leading to an increase in concentration of the second messenger molecule cyclic adenosine monophosphate (cAMP).

INDIGO's Reporter Cells contains an engineered luciferase reporter gene functionally linked to tandem Cyclic AMP Response Elements (CRE) and a minimal promoter. Activated adenylate cyclase results in the production of cAMP, which binds the transcription factor CREB (cAMP Response Element-Binding Protein). Activated CREB binds to CRE sequences, seeding the formation of a complete transcription complex that drives luciferase gene expression. Quantifying relative changes in luciferase enzyme activity in the treated reporter cells relative to the untreated reporter cells provides a sensitive surrogate measure of drug-induced changes in GIPR activity. Accordingly, the principal application of this reporter assay is in the screening of test compounds to quantify any functional activities, either activating or inhibitory, that they may exert against GIPR.

INDIGO’s Reporter Cells are transiently transfected and prepared as frozen stocks using a proprietary CryoMite™ process. This cryo-preservation method allows for the immediate dispensing of healthy, division-competent reporter cells into assay plates. There is no need for intermediate treatment steps such as spin-and-rinse of cells, viability determinations or cell titer adjustments prior to assay setup.

This assay kit provides the convenience of an all-inclusive cell-based reporter assay. In addition to GIPR Reporter Cells, provided are two optimized media for use in recovering the cryopreserved cells and for diluting test samples, the reference activator GIP, Luciferase Detection Reagents, and a cell culture-ready assay plate. [INDIGO Catalog Nos. IB38001 | IB38002]

WARNING This product is not for human or veterinary use.