INT-777
Cat. No.：YN321013
CAS No. ：1199796-29-6
| 产品名称: | INT-777 |
| CAS No.: | 1199796-29-6 |
| Chemical Name: | (3α,5β,6α,7α,12α,23S)-6-ethyl-3,7,12-trihydroxy-cholane-23-carboxylic acid |
| Synonyms: | S-EMCA |
| 分子量: | 450.65 |
| 分子式: | C₂₇H₄₆O₅ |
| SMILES: | O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@@H]4[C@H](C)C[C@H](C)C(O)=O)([H])C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | INT-777是有效的TGR5激动剂，EC50为 0.82 μM。 |
| IC50和靶点: | |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Schaap, F.G., Trauner, M., and Jansen, P.L.M.Bile acid receptors as targets for drug developmentNat. Rev. Gastroenterol. Hepatol.11(1),55-67(2014)
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 diabesityJ. Med. Chem.52(24),7958-7961(2009)
Thomas, C., Gioiello, A., Noriega, L., et al.TGR5-mediated bile acid sensing controls glucose homeostasisCell Metab.10(3),167-177(2009)
Kumar, D.P., Rajagopal, S., Mahavadi, S., et al.Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic ß cellsBiochem. Biophys. Res. Commun.427(3),600-605(2012)
Pols, T.W.H., Nomura, M., Harach, T., et al.TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loadingCell Metab.14(6),747-757(2011)
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 cellsAm. J. Physiol. Lung. Cell. Mol. Physiol.307(5),L407-L418(2014)
