EMD527040

EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research In Vitro EMD527040 inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins (IC50 50 ). EMD527040 inhibits the attachment of αvβ6 expressing cells (UCLAP3 cells) to fibronectin at IC 50 of 1.6 μM, as compared to >50 μM for αvβ3 and αvβ5 integrins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:αvβ6 6 nM (IC 50 )

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