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851333-14-7

851333-14-7 structure
851333-14-7 structure
  • Name: EMD527040
  • Chemical Name: EMD527040
  • CAS Number: 851333-14-7
  • Molecular Formula: C29H32Cl2N4O5
  • Molecular Weight: 587.49
  • Catalog: Signaling Pathways Cytoskeleton Integrin
  • Create Date: 2021-09-05 18:04:47
  • Modify Date: 2024-01-09 17:05:38
  • EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research[1].

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

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].
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.
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.

[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

Molecular Formula C29H32Cl2N4O5
Molecular Weight 587.49