GLP-1R Reporter Assay System (mouse)

This is an all-inclusive cell-based luciferase reporter assay kit targeting the Mouse Glucagon-Like Peptide-1 Receptor (GLP-1R). INDIGO's GLP-1R reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the GLP-1R. In addition to GLP-1R 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 GLP-1R. 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 Mouse Receptor Form Hybrid Assay Mode Agonist, Antagonist Kit Components mGLP-1R Reporter Cells Cell Recovery Medium (CRM) Compound Screening Medium (CSM) Glucagon-like Peptide-1, (7-36), (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 This assay utilizes proprietary cells that provide constitutive expression of the Mouse Glucagon-like Peptide-1 Receptor (mGLP-1R). The GLP-1R belongs to a class B G protein-coupled Receptor (GPCR), which is activated by several forms of GLP-1. GLP-1 is the second incretin hormone identified in the intestinal epithelial endocrine L-cells, followed by gastric inhibitory polypeptide (GIP). GLP-1/GLP-1R mainly regulates insulin secretion in response to high blood glucose levels. This receptor system plays a crucial role in energy homeostasis. Upon the ligand binding of GLP-1, GLP-1R signals through Galphas to drive an increase in intracellular cAMP via activation of adenylate cyclase (AC). This signaling pathway continues through the activation of protein kinase A (PKA) and exchange protein activated cAMP (EPAC) dependent mechanisms. Ultimately, the signal transduction cascade stimulates the opening of calcium and cation channels to induce calcium influx, which promotes insulin secretion. cAMP response binding element (CREB) is also activated by GLP-1R to induce the expression of insulin transcription factor in cAMP/PKA-dependent manner. Because of the significant role of GLP-1/GLP-1R as a key regulator of metabolism, several clinical trials have been attempted to develop therapies for patients with Type II diabetes. For example, GLP-1R agonists (GLP-1RAs) have been introduced as a novel class of therapeutic agent to manage glycemic control. 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 mGLP-1R 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 mGLP-1R. Protein function: G-protein coupled receptor for glucagon-like peptide 1 (GLP- 1) (PubMed:9568699). Ligand binding triggers activation of a signaling cascade that leads to the activation of adenylyl cyclase and increased intracellular cAMP levels. Plays a role in regulating insulin secretion in response to GLP-1 (PubMed:9568699). [The UniProt Consortium]