TGR5 (GP-BAR1) Reporter Assay Ki

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TGR5 (GP-BAR1) Reporter Assay Kit

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Cat No: 601440

Assay Kits - Cell-Based Assays

Bile acids are a diverse class of amphipathic molecules originally formed in liver and modified by microorganisms in the intestine. In addition to their conventional role in dietary lipid absorption, bile acids have been recognized as signaling molecu...

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Territorial Availability: Available through Bertin Technologies only in France

Correlated keywords:

GPBAR GPBAR1 luminescence TGR-5 HEK-293

Product Overview:
Bile acids are a diverse class of amphipathic molecules originally formed in liver and modified by microorganisms in the intestine. In addition to their conventional role in dietary lipid absorption, bile acids have been recognized as signaling molecules that regulate the synthesis and metabolism of bile acids, glucose homeostasis, and energy expenditure. The G protein-coupled membrane receptor for bile acid (TGR5 or GP-BAR1) is the most extensively studied receptor for bile acids. Activation of TGR5 by agonists leads to increase in intracellular cAMP, which signals the reduction of inflammatory cytokine expression in macrophage, increase of glucagon-like peptide (GLP-1) secretion in intestine, and energy expenditure in brown adipose tissue and muscle. Therefore, it has been an interesting drug target in metabolism and inflammation. Cayman's TGR5 (GP-BAR1) Reporter Assay Kit consists of a 96-well plate coated with a transfection complex containing DNA constructs for expressing TGR5 and a cAMP response element regulated secreted alkaline phosphatase (SEAP) reporter (TGR5 Reverse Transfection Strip Plate). Cells grown on the transfection complex will express TGR5 at the cell surface within 24 hours. Binding of agonists to TGR5 initiates a signal transduction cascade through the GαS and adenylate cyclase pathway resulting in the expression of SEAP which is secreted into the cell culture medium. Aliquots of culture medium are collected at 6-8 hours after stimulation, and SEAP activity is measured following the addition of a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is easy to use and can be readily applied to high-throughput screening for therapeutic compounds regulating activation of TGR5. A selective synthetic agonist, the TGR5 Receptor Agonist (3-[2-chlorophenyl]-N-[4-chlorophenyl]-N,5-dimethyl-4-isoxazolecarboxamide), is included in the kit for use as a positive control.{27533} The kit provides sufficient reagent to measure SEAP activity at three time points using the three included white assay plates.

Size	96 wells
Shipping	dry ice
Custom Code	3822.19
UNSPSC code	41116104

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.