EMD527040 is a powerful and highly specific αvβ6 antagonist, exhibiting notable antifibrotic properties. It is suitable for conducting research on carcinoma and liver fibrosis.

αvβ6 integrin:6 nM (IC50)

EMD527040 demonstrates selective inhibition, impeding the binding of recombinant αvβ6 to fibronectin with an IC50 of 6 nM, significantly more effective than its action on αvβ3 and αvβ5 integrins, which exhibit IC50 values of >9.5 μM. Furthermore, it inhibits the attachment of αvβ6-expressing cells (UCLAP3 cells) to fibronectin with an IC50 of 1.6 μM, a potency markedly higher than that observed for αvβ3 and αvβ5 integrins, where IC50 values exceed 50 μM[1].

EMD527040, administered through intraperitoneal injection at dosages ranging from 20-60 mg/kg from the second to the sixth week post-bile duct ligation (BDL), significantly mitigates bile ductular proliferation and peri-biliary collagen accumulation by 40-50%. It concurrently downregulates fibrogenic genes while upregulating fibrolytic genes, leading to improved liver structure and functionality. In addition, EMD527040 markedly decreased liver and spleen weights by 22% and 50%, respectively, in Mdr2(Abcb4) -/- mice. This was observed in a study employing adult male Wistar rats, showcasing amelioration of fibrosis progression in rodents afflicted with biliary fibrosis[Wistar rats, 20-60 mg/kg, intraperitoneal injection, weeks 2-6 post-BDL].