| 货号 | 16291-1mg |
| 描述 | TGR5 is a G protein-coupled receptor for bile acids that mediates energy balance, inflammation, and digestion.1 TGR5 Receptor Agonist is a synthetic small molecule activator of this bile acid receptor (pEC50 = 6.8-7.5) that is reported to improve glucagon-like peptide-1 (GLP-1) secretion by increasing intracellular cAMP levels viaTGR5.2,3 In a canine model, 1 mg/kg of this TGR5 receptor agonist co-administered with glucose has been shown to increase GLP-1 secretion, improving glucose disposal.2 This compound potently stimulates cAMP formation (EC50 = 2.3 pM) in HEK cells expressing TGR5, and has been used to investigate the signaling, trafficking, and regulation of TGR5 receptors in order to identify potentially useful therapeutics for metabolic disorders.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kawamata, Y.,Fujii, R.,Hosoya, A., et al. A G protein-coupled receptor responsive to bile acids. The Journal of Biological Chemisty 278(11), 9435-9440 (2003). 2.Evans, K.A.,Budzik, B.W.,Ross, S.A., et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. Journal of Medicinal Chemistry 52(24), 7962-7965 (2009). 3.Budzik, B.W.,Evans, K.A.,Wisnoski, D.D., et al. Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists. Bioorganic & Medicinal Chemistry Letters 20(4), 1363-1367 (2010). 4.Jensen, D.D.,Godfrey, C.B.,Niklas, C., et al. The bile acid receptor TGR5 does not interact with β-arrestins or traffic to endosomes but transmits sustained signals from plasma membrane rafts. The Journal of Biological Chemisty 288(32), 22942-22960 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 361.2 |
| 分子式 | C18H14Cl2N2O2 |
| CAS号 | 1197300-24-5 |
| 稳定性 | ≥ 2 years |
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