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PH-002 Sale

目录号 : GC31139

An inhibitor of ApoE4 domain interactions

PH-002 Chemical Structure

Cas No.:1311174-68-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,265.00
现货
5mg
¥1,170.00
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10mg
¥1,980.00
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25mg
¥4,320.00
现货
50mg
¥7,380.00
现货
100mg
¥8,357.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Cell experiment:

Neuro-2a cells stably expressing apoE3 or apoE4 are seeded at 7500-8000 cells/well on PLlysine-coated 24-well plates containing Opti-MEM with either 0.03% DMSO (control) or DMSO plus compound PH-002 (100 nM)[1].

References:

[1]. Brodbeck J, 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 May 13;286(19):17217-26.
[2]. Chen HK, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66.

产品描述

PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC50 = 116 nM in a FRET reporter assay for domain interaction).1,2 It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC50 = <1 nM).1

1.Chen, H.-K., Liu, Z., Meyer-Franke, A., et al.Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neuronsJ. Biol. Chem.287(8)5253-5266(2012) 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 correctorsJ. Biol. Chem.286(19)17217-17226(2011)

Chemical Properties

Cas No. 1311174-68-1 SDF
Canonical SMILES O=C(N1CCN(CC2=CC=C(NC(CC3=NN(C)C(C4=C3C=CC=C4)=O)=O)C=C2)CC1)OC(C)(C)C
分子式 C27H33N5O4 分子量 491.58
溶解度 DMSO : ≥ 75 mg/mL (152.57 mM) 储存条件 Store at -20°C
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1 mM 2.0343 mL 10.1713 mL 20.3426 mL
5 mM 0.4069 mL 2.0343 mL 4.0685 mL
10 mM 0.2034 mL 1.0171 mL 2.0343 mL
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