Description
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research.
Product information
CAS Number: 851333-14-7
Molecular Weight: 587.49
Formula: C29H32Cl2N4O5
Chemical Name: 3-[(2S)-3-(benzyloxy)-2-{5-[(pyridin-2-yl)amino]pentanamido}propanamido]-3-(3, 5-dichlorophenyl)propanoic acid
Smiles: OC(=O)CC(NC(=O)[C@H](COCC1C=CC=CC=1)NC(=O)CCCCNC1=CC=CC=N1)C1C=C(Cl)C=C(Cl)C=1
InChiKey: JHJAHOCSWUTJGR-BBMPLOMVSA-N
InChi: InChI=1S/C29H32Cl2N4O5/c30-22-14-21(15-23(31)16-22)24(17-28(37)38)35-29(39)25(19-40-18-20-8-2-1-3-9-20)34-27(36)11-5-7-13-33-26-10-4-6-12-32-26/h1-4,6,8-10,12,14-16,24-25H,5,7,11,13,17-19H2,(H,32,33)(H,34,36)(H,35,39)(H,37,38)/t24?,25-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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). 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.
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.
Products are for research use only. Not for human use.
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