Human GCGR Reporter Assay Kit

SIZE	SKU	PRICE
1 x-96 well format assays	IB45001	—
3 x-32 assays in-96 well format	IB45001-32	—

SIZE	SKU
1 x-96 well format assays	IB45001
3 x-32 assays in-96 well format	IB45001-32

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Specifications
Data
Target Background
Documentation
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Product Description and Product Data

This is an all-inclusive cell-based luciferase reporter assay kit targeting the the Human Glucagon Receptor (GCGR). INDIGO’s GCGR reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the GCGR. In addition to GCGR 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 GCGR. 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 GCGR Reporter Cells Cell Recovery Medium (CRM) Compound Screening Medium (CSM) Glucagon HCl (30 uM) 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 GCGR. Activation assays were performed using the reference compound Glucagon HCl (provided), Retatrutide, Survodutide and Mazdutide (all from Cayman Chemical, Ann Arbor, MI).

Inhibition of GCGR. GCGR reporter cells were co-treated with an EC80 concentration of the reference activator Glucagon HCl and varying concentrations of GCGR Antag 4 (Cayman Chemical, Ann Arbor, MI). INDIGO’s Live Cell Multiplex (LCM) Assay confirmed that no treatment concentrations were cytotoxic (data not shown).

Target Background

Glucagon is a linear peptide containing 29 amino acids. It is secreted by islet α cells and mainly targets liver cells. Glucagon Receptor (GCGR) is a G-Protein-Coupled Receptor (GPCR) mainly detected in islet β cells and liver cells. After glucagon binds to GCGR, it promotes liver glycogen breakdown and increases blood glucose levels to stimulate insulin release. GCGR belongs to the class B GPCR superfamily and signals through Gαs/adenylyl cyclase activation, leading to an increase in concentration of the second messenger molecule cyclic adenosine monophosphate (cAMP).

The role of GCGR in the development of type 1 and type 2 diabetes (T1D, T2D) remains controversial, as conflicting evidence exists. However, each type of diabetes in animals and humans is associated with hypoglucagonemia.

Obesity is a chronic, treatable, neurometabolic disease that is projected to affect nearly a quarter of the world population by 2035. Novel therapeutics that engage with one or more of the GPCR targets, for example GCGR, GIPR and GLP-1R, have displayed positive results in regulating body-fat mass and energy homeostasis. Retatrutide, for example, is a single peptide conjugated to a fatty diacid moiety and has agonism toward GCGR, GIPR and GLP-1R. In recent phase 1b trials, treatment with Retatrutide led to a 10% weight reduction compared to a placebo control. GCGR, GIPR, and GLP-1R therefore continue to command considerable interest in therapeutic development and drug safety screening.