TGR5 (GP-BAR1) Reporter Assay Kit
- CAS No.
- Chemical Name:
- TGR5 (GP-BAR1) Reporter Assay Kit
- Synonyms
- TGR5 (GP-BAR1) Reporter Assay Kit
- CBNumber:
- CB54815313
- Molecular Formula:
- Molecular Weight:
- 0
- MDL Number:
- MOL File:
- Mol file
TGR5 (GP-BAR1) Reporter Assay Kit price More Price(1)
TGR5 (GP-BAR1) Reporter Assay Kit Chemical Properties, Uses, Production
Description
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-
References
[1] KAREN A. EVANS*. Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists[J]. Journal of Medicinal Chemistry, 2009, 52 24: 7962-7965. DOI: 10.1021/jm901434t
TGR5 (GP-BAR1) Reporter Assay Kit Preparation Products And Raw materials
Raw materials
Preparation Products
TGR5 (GP-BAR1) Reporter Assay Kit Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Cayman Chemical Company | -- | sales@caymanchem.com | China | 6808 | 58 |
| Shenzhen Campbell Biotechnology Co., Ltd. | -- | CHINA | 6891 | 58 | |
| Langfang Yusheng Ruichuang Technology Co., Ltd. | -- | CHINA | 1857 | 58 | |
| Cayman Chemical Company | -- | cayman@caymanchem.com | United States | 6987 | 81 |
| Supplier | Advantage |
|---|---|
| Cayman Chemical Company | 58 |
| Shenzhen Campbell Biotechnology Co., Ltd. | 58 |
| Langfang Yusheng Ruichuang Technology Co., Ltd. | 58 |
| Cayman Chemical Company | 81 |
