产品说明书

PH-002

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Chemical Structure| 1311174-68-1 同义名 : -
CAS号 : 1311174-68-1
货号 : A1176916
分子式 : C27H33N5O4
纯度 : 99%+
分子量 : 491.582
MDL号 : MFCD22666400
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 80 mg/mL(162.74 mM),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 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
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

[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.