851333-14-7

Name	β-Alanine, N-[1-oxo-5-(2-pyridinylamino)pentyl]-O-(phenylmethyl)-L-seryl-3-(3,5-dichlorophenyl)-
CAS	851333-14-7
Molecular Formula	C29H32Cl2N4O5
Molecular Weight	587.5
MOL File	851333-14-7.mol

Synonyms

EMD527040 β-Alanine, N-[1-oxo-5-(2-pyridinylamino)pentyl]-O-(phenylmethyl)-L-seryl-3-(3,5-dichlorophenyl)-

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Chemical Properties

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

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

Supplier

Shanghai?Medlife?Pharm-Tech?Co.,?Ltd

Telephone021-59167510 18117107507

Websitehttps://www.med-life.cn/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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