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EMD527040

Chemical Structure : EMD527040

CAS No.: 851333-14-7

EMD527040

Catalog No.: PC-49394Not For Human Use, Lab Use Only.

EMD527040 (EMD 527040) is a potent, specific, nonpeptidic inhibitor of αvβ6 integrin, inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

EMD527040 (EMD 527040) is a potent, specific, nonpeptidic inhibitor of αvβ6 integrin, inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins.
EMD527040 attenuated bile ductular proliferation and peribiliary collagen deposition by 40%-50%, induced down-regulation of fibrogenic and up-regulation of fibrolytic genes, and improved liver architecture and function.
EMD527040 reduced activated cholangiocyte proliferation, their adhesion to fibronectin, and endogenous activation of TGF-beta1 by 50% but did not affect bile duct apoptosis.
EMD527040 reduced expression of profibrotic markers and reduced fibrosis formation in DSG2-W2A mutation in arrhythmogenic cardiomyopathy (ACM) animal model.

Physicochemical Properties

M.Wt 587.498
Formula C29H32Cl2N4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-{(S)-3-Benzyloxy-2-[5-(pyridin-2-ylamino)-pentanoylamino]-propionylamino}-3-(3,5-dichloro-phenyl)-propionic acid

References

1. Goodman SL, et al. J Med Chem. 2002;45:1045-1051.

2. Patsenker E, et al. Gastroenterology. 2008 Aug;135(2):660-70.

3. Camilla Schinner, et al. Circulation. 2022 Oct 21. doi: 10.1161/CIRCULATIONAHA.121.057329.

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