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TR-14035
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TR-14035图片
CAS NO:232271-19-1
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 474.33
Formula C24H21Cl2NO5
CAS No. 232271-19-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 41 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES O=C(O)[C@H](CC1=CC=C(C2=C(OC)C=CC=C2OC)C=C1)NC(C3=C(Cl)C=CC=C3Cl)=O
Synonyms TR-14035; TR14035; TR 14035
实验参考方法
In Vitro

In vitro activity: TR-14035 is a novel, dual antagonist of alpha4beta7 integrin with IC50 of 7 nM and alpha4beta1 integrin with IC50 of 87 nM. TR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 2.93 and 0.75 nM, respectively. It inhibited binding of soluble ligands to alpha(4)beta(1) or alpha(4)beta(7) on cells of human or rodent origin with similar potency. Under shear flow in vitro. TR-14035 (IC(50) alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM) has completed Phase I studies in Europe.


Kinase Assay: TR-14035 is a novel, dual antagonist of alpha4beta7 integrin with IC50 of 7 nM and alpha4beta1 integrin with IC50 of 87 nM.


Cell Assay:

In VivoTR14035 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
Animal model
Formulation & Dosage
References J Pharmacol Exp Ther. 2002 Jul;302(1):153-62; Bioorg Med Chem. 2002 Jun;10(6):2051-66.