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PE859

目录号: PL07214 纯度: ≥99%

PE859是tau和Aβ积累的有效抑制剂，IC50值分别为0.66 和1.2 μM。

CAS No. :1402727-29-0

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中文名称	PE859
中文别名	PE-859;PE 859;PE859游离态;化合物PE859
英文名称	PE859
英文别名	PE859;AMBZHNVCLPHAKA-NSJFVGFPSA-N;PE-859; PE 859;1H-Indole, 6-[(1E)-2-[5-[(1E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-3-yl]ethenyl]-
Cas No.	1402727-29-0
分子式	C₂₈H₂₄N₄O₂
分子量	448.52
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	PE859是tau和Aβ积累的有效抑制剂，IC50值分别为0.66 和1.2 μM。

产品详情	PE859是tau和Aβ积累的有效抑制剂，IC₅₀值分别为0.66 和1.2 μM。
生物活性	PE859 is a potent inhibitor of both tau and Aβ aggregation with IC 50 values of 0.66 and 1.2 μM, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 0.66 μM (tau), 1.2 μM (Aβ)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (111.48 mM; Need ultrasonic)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

PE859

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