| 产品描述： | PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively. |
| 靶点： |
IC50: 0.66 μM (tau), 1.2 μM (Aβ);BetaAmyloid; Gamma-secretase; MicrotubuleAssociated |
| 体外研究： |
PE859 inhibits the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner. In each assay, the IC50 values calculated at the last measurement periods are 0.81 μM, and 2.23 μM, respectively. PE859 inhibits tau aggregation through formation of beta-sheet structure |
| 体内研究： |
PE859 could cross the blood-brain barrier and that PE859 could be distributed into the tissues of the central nervous system. The maximum concentration of PE859 is 2.005 μg/mL in the blood at 3 h and 1.428 μg/g in the brain at 6 h. PE859 delays onset and progression of the motor dysfunction in JNPL3 mice. PE859 delays progression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau. |
| 参考文献： |
1. Okuda M, et al. Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5024-5028. 2. Okuda M, et al. PE859, a novel tau aggregation inhibitor, reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e0117511. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.23 ml |
11.148 ml |
22.296 ml |
| 5 mM |
0.446 ml |
2.23 ml |
4.459 ml |
| 10 mM |
0.223 ml |
1.115 ml |
2.23 ml |
| 50 mM |
0.045 ml |
0.223 ml |
0.446 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)
