GIPR Reporter Assay System (human)

This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Gastric Inhibitory Polypeptide Receptor (GIPR). INDIGO's GIPR reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the GIPR. In addition to OXTR Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user's test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against GIPR. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture. Features Clear, Reproducible Results All-Inclusive Assay Systems Exceptional Cell Viability Post-Thaw Consistent Results Lot to Lot Product Specifications Target Type: GPCR Species: Human Receptor Form: Hybrid Assay Mode: Agonist, Antagonist Kit Components: Human GIPR Reporter Cells Cell Recovery Medium (CRM) Compound Screening Medium (CSM) GIP, (ref. agonist, in PBS+0.1%BSA) Detection Substrate Detection Buffer White, sterile, cell-culture ready assay plate Shelf Life: 6 months Shipping Requirements: Dry Ice Storage temperature: -80C. Target Background 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 beta-cells. GIPR belongs to the class B1 G protein-coupled receptor (GPCR) superfamily and signals through Galphas/adenylyl cyclase activation, leading to an increase in concentration of the second messenger molecule cyclic adenosine monophosphate (cAMP). Historically, GLP-1R agonists have shown clinical success in treating obesity and type 2 diabetes (T2D). GIP, and its receptor GIPR, are also associated with the pathophysiology of obesity and T2D. As such, GIPR is an important therapeutic target. As an example, the anti-obesity injectable drug Tirzepatide is a single-molecule co-activator of GLP-1R and GIPR. Clinical studies for this compound showed efficacy for glucose lowering and weight loss in T2D patients as compared to control groups. Interestingly, Tirzepatide displayed higher affinity for GIPR compared to GLP-1R, with signaling studies demonstrating similar action as the native GIP peptide. GIPR and GLP-1R continue to command considerable interest in therapeutics development and drug safety screening. Protein function: This is a receptor for GIP. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. [The UniProt Consortium]