|4-(4-(2-(3-甲基-4-氧代-3,4-二氢酞嗪-1-基)乙酰氨基)苄基)哌嗪-1-甲酸叔丁酯|CsnPharm

CAS No.: 1311174-68-1

PH-002 Catalog No. CSN24778

Synonyms: PH-002

PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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].
参考文献

[1] Corder EH, Saunders AM, Strittmatter WJ, et al. Gene dose of apolipoprotein E type 4 allele and the risk of Alzheimer's disease in late onset families. Science. 1993;261(5123):921–923.
[2] Brodbeck J, McGuire J, Liu Z, et al. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011;286(19):17217–17226.
[3] Chen HK, Liu Z, Meyer-Franke A, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012;287(8):5253–5266.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0342 mL
- 10.1712 mL
- 20.3425 mL
- 5 mM
- 0.4068 mL
- 2.0342 mL
- 4.0685 mL
- 10 mM
- 0.2034 mL
- 1.0171 mL
- 2.0342 mL

技术信息

CAS号

1311174-68-1

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H33N5O4

运输

蓝冰

分子量

491.58

别名

PH-002

溶解度

DMSO	75.0 mg/mL (152.6 mM)
Water	insoluble

动物实验配方

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PH-002 Catalog No. CSN24778

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