1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPE859Cat. No.: HY-12662CAS No.: 1402727-29-0分式: CHNO分量: 448.52作靶點: Microtubule/Tubulin作通路: Cell Cycle/DNA Damage; Cytoskeleton儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 50 mg/mL (111.4

2、8 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.57 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.57 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 PE859是tau和A積累的有效抑制劑，IC50值分別為0.66 和1.2

3、M。IC50 & Target IC50: 0.66 M (tau), 1.2 M (A) 1體外研究 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 M,and 2.23 M, respectively. PE859 inhibits tau

4、aggregation through formation of beta-sheet structure 2.體內研究 PE859 could cross the blood-brain barrier and that PE859 could be distributed into the tissues of the centralnervous system. The maximum concentration of PE859 is 2.005 g/mL in the blood at 3 h and 1.428 g/g inthe brain at 6 h. PE859 delay

5、s onset and progression of the motor dysfunction in JNPL3 mice. PE859 delaysprogression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau. 2PROTOCOLKinase Assay 2 Tau aggregation is monitored using thioflavin T. The test compound (PE859), 10 M 3RMBD and 10 Mhe

6、parin are dissolved in 50 mM Tris-HCl (pH7.6), and incubated at 37C up to 144 hours. At each point ofincubation time, 135 L of the solutions are removed and mixed with 15 L of 100 M ThT solution (finalconcentration: 10 M) and the fluorescence intensity with excitation at 440 nm and emission at 486 n

7、m ismeasured 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: PE859 is dissolved in 80% PEG400 and 20% water solution at 5 mg/mL, and orally-administered at aAdministration 2 dose of 40 mg/kg/day for 6 months (from 9 to 15 months of age).

8、The body weights of the mice are measuredonce a week during PE859 treatment 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發表的科研獻 Elife. 2019 Mar 25;8. pii: e45457.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Okuda M, et

9、 al. Design and synthesis of curcumin derivatives as tau and amyloid 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 neuraldysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e0117511.McePdfHeig t Caution: Product has not been fully validated for medi