化合物PE859 T4077

Product Introduction
Bioactivity


英文名: PE859

描述: PE859 是 tau 和 Aβ 聚集的有效抑制剂，IC50值分别为 0.66 和 1.2 μM。

激酶实验: PEL cells are incubated in triplicate in a 96-well microculture plate in the presence of different concentrations of methyl-β-cyclodextrin (0-10 mM) in a final volume of 0.1 mL for 24 h at 37°C. Subsequently, MTT (0.5 mg/mL final concentration) is added to each well. After 3 h of additional incubation, 100 μL of a 0.04 N HCl is added to dissolve the crystals. Absorption values at 570 nm are determined.

体外活性: In an Alzheimer's patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid β (Aβ) peptide and Tau Protein, are observed as the two major hallmarks of this disease. 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 the formation of a beta-sheet structure[2].

体内活性: PE859 is able to cross the blood-brain barrier and thus 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. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 30 mg/mL


关键字: PE 859 | Inhibitor | PE859 | PE-859 | inhibit | Microtubule/Tubulin

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相关库: Anti-Neurodegenerative Disease Compound Library | Microtubule-Targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Protease Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Alzheimer's Disease Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途