| 货号 | 17678-1mg |
| 描述 | TGR5 is a transmembrane G protein-coupled receptor that is activated by bile acid.1 INT-777 is a semisynthetic bile acid that acts as an agonist of TGR5 (EC50 = 0.82 µM).2,3 It is active in vivo, stimulating the secretion of glucagon-like peptide 1 (GLP-1) in mice when given orally (30 mg/kg) after a glucose challenge, particularly when given with a dipeptidyl-peptidase-4 inhibitor.3 INT-777 increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to diet-induced obesity.3 It also stimulates insulin secretion in pancreatic β-cells, reduces inflammation and inhibits atherosclerosis in mice, and promotes chloride secretion through cystic fibrosis transmembrane conductance regulator (CFTR) in Calu-3 airway epithelial cells.4,5,6 |
| 别名 | 6-EMCA;S-EMCA;HY-15677; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Schaap, F.G.,Trauner, M. and Jansen, P.L.M. Bile acid receptors as targets for drug development. Nat. Rev. Gastroenterol. Hepatol. 11, 55-67 (2014). 2.Pellicciari, R.,Gioiello, A.,Macchiarulo, A., et al. Discovery of 6α-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. Journal of Medicinal Chemistry 52(24), 7958-7961 (2009). 3.Thomas, C.,Gioiello, A.,Noriega, L., et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metabolism 10, 167-177 (2009). 4.Kumar, D.P.,Rajagopal, S.,Mahavadi, S., et al. Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic ß cells. Biochemical and Biophysical Research Communications 427(3), 600-605 (2012). 5.Pols, T.W.H.,Nomura, M.,Harach, T., et al. TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. Cell Metabolism 14, 747-757 (2011). 6.Hendrick, S.M.,Mroz, M.S.,Greene, C.M., et al. Bile acids stimulate chloride secretion through CFTR and calcium-activated Cl- channels in Calu-3 airway epithelial cells. American Journal of Physiology.Regulatory, Integrative and Comparative Physiology 307(5), L407-L418 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 450.7 |
| 分子式 | C27H46O5 |
| CAS号 | 1199796-29-6 |
| 稳定性 | ≥ 2 years |
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