For research use only. Not for therapeutic Use.
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research[1].
EMD527040 inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins (IC5050)[1].EMD527040 inhibits the attachment of αvβ6 expressing cells (UCLAP3 cells) to fibronectin at IC50 of 1.6 μM, as compared to >50 μM for αvβ3 and αvβ5 integrins[1].
EMD527040 (intraperitoneal injection; 20-60 mg/kg; week 2 to 6 after BDL) attenuates bile ductular proliferation and peribiliary collagen deposition by 40-50%, induces downregulation of fibrogenic and upregulation of fibrolytic genes, and improves liver architecture and function. EMD527040 significantly reduced liver and spleen weights by 22% and 50%, respectively in Mdr2(Abcb4)-/- mice[1].
| Catalog Number | I045695 |
| CAS Number | 851333-14-7 |
| Synonyms | 3-(3,5-dichlorophenyl)-3-[[(2S)-3-phenylmethoxy-2-[5-(pyridin-2-ylamino)pentanoylamino]propanoyl]amino]propanoic acid |
| Molecular Formula | C29H32Cl2N4O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H32Cl2N4O5/c30-22-14-21(15-23(31)16-22)24(17-28(37)38)35-29(39)25(19-40-18-20-8-2-1-3-9-20)34-27(36)11-5-7-13-33-26-10-4-6-12-32-26/h1-4,6,8-10,12,14-16,24-25H,5,7,11,13,17-19H2,(H,32,33)(H,34,36)(H,35,39)(H,37,38)/t24?,25-/m0/s1 |
| InChIKey | JHJAHOCSWUTJGR-BBMPLOMVSA-N |
| SMILES | C1=CC=C(C=C1)COCC(C(=O)NC(CC(=O)O)C2=CC(=CC(=C2)Cl)Cl)NC(=O)CCCCNC3=CC=CC=N3 |
| Reference | [1]. Eleonora Patsenker, et al. Inhibition of integrin alphavbeta6 on cholangiocytes blocks transforming growth factor-beta activation and retards biliary fibrosis progression. Gastroenterology. 2008 Aug;135(2):660-70. [2]. Yury Popov, et al. Integrin alphavbeta6 is a marker of the progression of biliary and portal liver fibrosis and a novel target for antifibrotic therapies. J Hepatol |
