TR-14035

公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!

抑制剂描述：

产品名称：TR-14035

产品别名：见爱必信官网

英文别名：TR-14035

靶点：Integrin

CAS：232271-19-1

纯度：98%

外观：见爱必信官网

保存方法：Store at -20°C

描述：

TR-14035 is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

溶解性：DMSO : ≥ 41 mg/mL (86.44 mM)

体外研究：

TR-14035 (IC50: alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM) has completed Phase I studies in Europe. 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. OATP1B1/OATP-C and OATP1B3/OATP8 expressed in oocytes mediated the TR-14035 uptake with K(m) of 7.5 and 5.3 microM, respectively. TR14035 blocked the binding of human alpha(4)beta(7) to a (125)I-MAdCAM-Ig fusion protein with IC(50) values of 0.75 nM. Under shear flow in vitro, 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.

体内研究：Biliary excretion and total body clearance of unchanged TR-14035 in EHBRs were significantly lower than those in normal rats, while there was no difference in the clearances between wild and mdr1a/b- or Bcrp-knockout mice . TR14035 blocked adhesion to HEVs (ED50: of 0.01-0.1 mpk i.v.) .

产品信息订购：

产品更多信息请进入爱必信网站咨询