PH-002
目录号: PL09195 纯度: ≥98%
CAS No. :1311174-68-1
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中文名称
PH-002
中文别名
4-[[[4-[[2-(3,4-二氢-3-甲基-4-氧代-1-酞嗪基)乙酰基]氨基]苯基]甲基]-1-哌嗪羧酸叔丁酯;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;化合物PH-002;1311174-68-1
英文名称
PH-002
英文别名
4-[[4-[[2-(3,4-Dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester;PH 002;PH002;PH-002;1-Piperazinecarboxylic acid, 4-[[4-[[2-(3,4-dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-, 1,1-dimethylethyl ester;PH-002 >=98% (HPLC);inhibit,PH 002,PH-002,Inhibitor,PH002
Cas No.
1311174-68-1
分子式
C27H33N5O4
分子量
491.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PH-002 是一种抑制载脂蛋白 (apo) E4 神经内分子相互作用的抑制剂,其 IC50 (FRET) 值为116 nM。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
116 nM (Apo E4 in FRET).
体外研究(In Vitro)
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells, with an IC50 of 116 nM in FRET. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PH-002 is also shown to increase COX1 levels in primary neurons from NSE-apoE4 transgenic mouse cortex and hippocampus. After 4 days of treatment with PH-002 (200 nM), COX1 levels are increased by ~60%. PH-002 (100 nM) increases dendritic spine development in primary neurons from NSE-apoE4 transgenic mice to levels comparable with those in NSE-apoE3 primary neurons (apoE3-expressing primary neurons treated with PH-002 gave results identical to untreated primary neurons). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : ≥ 75 mg/mL (152.57 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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