Human GIPR Reporter Assay Kit

SIZE	SKU	PRICE
1 x-384 well format assays	IB38002	—
1 x-96 well format assays	IB38001	—

SIZE	SKU
1 x-384 well format assays	IB38002
1 x-96 well format assays	IB38001

Specifications
Data
Target Background
Documentation
Overview
Citation
Related Products

Product Description and Product Data

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

Data

Activation of GIPR. Activation assays were performed using the reference polypeptides GIP (provided) and Tirzepatide. Luminescence was quantified and values of average (n=3) relative light units (RLU), corresponding standard deviation (SD), Fold- Activation, and Z’ values were calculated. GraphPad Prism software was used to plot data using the least-squares method of non-linear regression for Fold-Activation or RLU vs. Log10 [Cmpd, nM], and to determine EC50 / IC50 values.

Inhibition of GIPR. GIPR reporter cells were co-treated with an EC80 concentration of the reference activator GIP and varying concentrations of anti-GIPR specific monoclonal antibody (R&D System, Minneapolis, MN). INDIGO’s Live Cell Multiplex (LCM) Assay confirmed that no treatment concentrations were cytotoxic (data not shown). Luminescence was quantified and values of average (n=3) relative light units (RLU), corresponding standard deviation (SD), Fold- Activation, and Z’ values were calculated. GraphPad Prism software was used to plot data using the least-squares method of non-linear regression for Fold-Activation or RLU vs. Log10 [Cmpd, nM], and to determine EC50 / IC50 values.

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 β-cells.

GIPR belongs to the class B1 G protein-coupled receptor (GPCR) superfamily and signals through Gαs/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.