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TR-14035

  Cat. No.:  DC22292   Featured
Chemical Structure
232271-19-1
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More than 5000 active chemicals with high quality for research!
Field of application
TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 232271-19-1
Synonyms: TR-14035，TR 14035，TR14035
SMILES: COC1=C(C2=CC=C(C[C@@H](C(O)=O)NC(C3=C(Cl)C=CC=C3Cl)=O)C=C2)C(OC)=CC=C1
Formula: C24H21Cl2NO5
M.Wt: 474.33
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist TR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. TR14035 blocked binding of human alpha(4)beta(7)-expressing RPMI-8866 cells or murine mesenteric lymph node lymphocytes to MAdCAM-Ig with IC(50) values of 0.1 microM [2]. TR14035 blocked adhesion to HEVs [ED(50) of 0.01-0.1 mpk i.v.].TR-14035 was taken up by rat and human hepatocytes by an apparently single saturable mechanism with K(m) of 6.7 and 2.1 microM, respectively, and taurocholate and digoxin reduced this uptake [3].
Target: IC50 Value: alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM [1] Target: integrin
References: [1]. Sircar I, et al. Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha(4)beta(7)/alpha(4)beta(1) integrin antagonist. Bioorg Med Chem. 2002 Jun;10(6):2051-66. [2]. Egger LA, et al. Alpha(4)beta(7)/alpha(4)beta(1) dual integrin antagonists block alpha(4)beta(7)-dependent adhesion under shear flow. J Pharmacol Exp Ther. 2002 Jul;302(1):153-62.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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