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EMD527040 

Cat. No.: HY-101473
Handling Instructions

EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research.

For research use only. We do not sell to patients.

EMD527040 Chemical Structure

EMD527040 Chemical Structure

CAS No. : 851333-14-7

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Description

EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research[1].

IC50 & Target[1]

αvβ6

6 nM (IC50)

In Vitro

EMD527040 inhibits binding of recombinant αvβ6 to fibronectin at 6 nM as compared to >9.5 μM for αvβ3 and αvβ5 integrins (IC5050)[1].
EMD527040 inhibits the attachment of αvβ6 expressing cells (UCLAP3 cells) to fibronectin at IC50 of 1.6 μM, as compared to >50 μM for αvβ3 and αvβ5 integrins[1].

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[1].

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.
Molecular Weight

587.49

Formula

C₂₉H₃₂Cl₂N₄O₅

CAS No.
SMILES

O=C(O)CC(NC([[email protected]@H](NC(CCCCNC1=NC=CC=C1)=O)COCC2=CC=CC=C2)=O)C3=CC(Cl)=CC(Cl)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EMD527040EMD 527040EMD-527040IntegrinIntegrin αvβ6bile duct ligationBDLUCLAP3lung carcinoma,Liver fibrosisInhibitorinhibitorinhibit

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EMD527040
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HY-101473
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