| Identification | Back Directory | [Name]
β-Alanine, N-[1-oxo-5-(2-pyridinylamino)pentyl]-O-(phenylmethyl)-L-seryl-3-(3,5-dichlorophenyl)- | [CAS]
851333-14-7 | [Synonyms]
EMD527040
β-Alanine, N-[1-oxo-5-(2-pyridinylamino)pentyl]-O-(phenylmethyl)-L-seryl-3-(3,5-dichlorophenyl)- | [Molecular Formula]
C29H32Cl2N4O5 | [MOL File]
851333-14-7.mol | [Molecular Weight]
587.5 |
| Chemical Properties | Back Directory | [Boiling point ]
860.6±65.0 °C(Predicted) | [density ]
1.326±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
3.99±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
EMD527040 is a novel potent and highly selective αvβ6 antagonist. | [Uses]
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research[1]. | [in vivo]
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]. | Animal Model: | Male adult Wistar rats | | Dosage: | 20-60 mg/kg | | Administration: | Intraperitoneal?injection; 20-60 mg/kg; week 2 to 6 after BDL (bile duct ligation) | | Result: | Ameliorated fibrosis progression in rodents with biliary fibrosis. |
| [IC 50]
αvβ6: 6 nM (IC50) | [References]
[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. DOI:10.1053/j.gastro.2008.04.009
[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 DOI:10.1016/j.jhep.2007.11.021 |
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