PE859

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Chemical Structure| 1402727-29-0 同义名 : -
CAS号 : 1402727-29-0
货号 : A102932
分子式 : C28H24N4O2
纯度 : 99%+
分子量 : 448.516
MDL号 : MFCD28411710
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(111.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PE859 is a potent Aβ aggregation inhibitor with IC50 values of 1.2μM and 0.66μM for Aβ aggregation and Tau aggregation. PE859 exhibited improved pharmacokinetic profile and brain permeability through oral administration. A four-week oral administration of PE859 at doses of 20 and 40 mg/kg/day significantly reduced the amount of sarkosyl-insoluble tau in the brain of JNPL3 human tau P301L transgenic mice[3]. PE859 inhibited the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner with IC50 values of 0.81 μM and 2.23 μM, respectively, in in vitro assay. Oral administration of PE859 at dose of 40mg/kg/day for 6 months delayed onset and progression of the motor dysfunction and reduced the amount of sarcosyl-insoluble tau in the spinal cord of JNPL3 mice[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.11mL

22.30mL

4.46mL

2.23mL
参考文献

[1]Okuda M, Hijikuro I, 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, Hijikuro I, 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.

[3]Okuda M, Hijikuro I, Fujita Y, Teruya T, Kawakami H, Takahashi T, Sugimoto H. 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. doi: 10.1016/j.bmcl.2016.08.092. Epub 2016 Aug 31. PMID: 27624076.

[4]Okuda M, Hijikuro I, Fujita Y, Wu X, Nakayama S, Sakata Y, Noguchi Y, Ogo M, Akasofu S, Ito Y, Soeda Y, Tsuchiya N, Tanaka N, Takahashi T, Sugimoto H. 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. doi: 10.1371/journal.pone.0117511. PMID: 25659102; PMCID: PMC4319983.