GCGR Reporter Assay System (human)

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. Target Background Glucagon is a linear peptide containing 29 amino acids. It is secreted by islet alpha cells and mainly targets liver cells. Glucagon Receptor (GCGR) is a G-Protein-Coupled Receptor (GPCR) mainly detected in islet beta 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 Galphas/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. Protein function: G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system. [The UniProt Consortium]