生物活性 | |||
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描述 | Apolipoprotein (ApoE) is the major apolipoprotein in cerebrospinal fluid and is derived from the brain. Apolipoprotein E4 (apoE4) is the major genetic risk factor for late onset Alzheimer disease (AD), increasing the risk of developing AD at earlier ages of onset[1]. It has been suggested that domain interaction mediates a broad spectrum of apoE4 isoform-specific effects. PH-002 is an inhibitor of apoE4 intramolecular domain interaction in neuronal cells. Treatment with 100 nM of PH002 for 3 days rescued intracellular trafficking of apoE4, stimulated neurite outgrowth and increased the dendritic spine density in apoE4-expressing neuro-2a cells, which suggest a new strategy for developing anti-AD therapeutics targeting apoE4[2]. | ||
作用机制 | PH-002 directly binds to the apoE4 amino-terminal domain[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.03mL 0.41mL 0.20mL |
10.17mL 2.03mL 1.02mL |
20.34mL 4.07mL 2.03mL |
参考文献 |
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