| 产品描述： | TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases. |
| 靶点： |
α4β7:7 nM (IC50);α4β1:87 nM (IC50);Integrin |
| 体内研究： |
TR-14035 (3 mg/kg; i.g.) produces a significant decrease of the airways hyper-responsiveness to 5-hydroxytryptamine (5-HT) in an experimental model of allergic asthma in Brown Norway rats. TR-14035 exhibits moderate oral bioavailability (rat 17.1%, dog 13.2%) and Cmax (rat 0.18, dog 0.10 μg eq./mL) following oral administration (rat 10 and dog 10 mg/kg). TR-14035 exhibits terminal elimination half-lives (rat 0.28 h and, dog 0.81 h) due to high plasma clearance (3865 and 1664 mL/h/kg respectively) following intravenous administration (rat 3 mg/kg and dog 3 mg/kg) |
| 参考文献： |
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. 3. Julio Cortijo, et al. A small molecule, orally active, α4β1/α4β7 dual antagonist reduces leukocyte infiltration and airway hyper-responsiveness in an experimental model of allergic asthma in Brown Norway rats. Br J Pharmacol. 2006 Mar; 147(6): 661–670. 4. M Tsuda-Tsukimoto, et al. Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica |
| 溶解性： |
DMSO : ≥ 41 mg/mL (86.44 mM) |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.108 ml |
10.541 ml |
21.082 ml |
| 5 mM |
0.422 ml |
2.108 ml |
4.216 ml |
| 10 mM |
0.211 ml |
1.054 ml |
2.108 ml |
| 50 mM |
0.042 ml |
0.211 ml |
0.422 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京