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Itanapraced {[allProObj[0].p_purity_real_show]}

货号:A464388 同义名: CHF5074;CSP-1103

Itanapraced是一种γ-分泌酶调节剂,IC50值分别为3.6 μM和18.4 μM,能够减少Aβ42和Aβ40的分泌,可用于阿尔茨海默病的研究。

Itanapraced 化学结构 CAS号:749269-83-8
Itanapraced 化学结构
CAS号:749269-83-8
Itanapraced 3D分子结构
CAS号:749269-83-8
Itanapraced 化学结构 CAS号:749269-83-8
Itanapraced 3D分子结构 CAS号:749269-83-8
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Itanapraced 纯度/质量文件 产品仅供科研

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Itanapraced 生物活性

描述 Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. It reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively, and prevents cell apoptosis in hippocampal neurons caused by oxygen and glucose deprivation (OGD). Itanapraced is researched for potential use in Alzheimer's disease treatment[1][2].
体内研究

Itanapraced, when given orally at 375 ppm in the diet for 17 weeks, lowers both Aβ42 and Aβ40 levels and reduces brain plaque burden in Tg2576 transgenic mice[1].

体外研究

Itanapraced, at concentrations of 0.03-100 µM, inhibits Aβ secretion in human neuroglioma cells (H4swe) expressing APPswe with IC50 values of 3.6 μM for Aβ42 and 18.4 μM for Aβ40[1].

Itanapraced, at doses of 5-200 µM, inhibits Notch processing in HEK293swe cells with effective concentrations starting at 15 µM[1].

Itanapraced, in a range of 0-1000 µM over 30 minutes, dose-dependently suppresses action potentials with an IC50 of 106 μM[2].

Itanapraced, at concentrations ranging from 30-100 µM, dose-dependently reduces excitatory synaptic transmission[2].

Itanapraced, at doses of 1-10 µM, significantly diminishes cell apoptosis in hippocampal neurons caused by oxygen and glucose deprivation (OGD)[2].

Itanapraced 参考文献

[1]Imbimbo BP, et al. 1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretasemodulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease withoutcausing peripheral toxicity. J Pharmacol Exp Ther. 2007 Dec;323(3):822-830.

[2]Mango D, et al. Electrophysiological and metabolic effects of CHF5074 in the hippocampus: protection against in vitro ischemia. Pharmacol Res. 2014 Mar;81:83-90.

Itanapraced 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.38mL

3.08mL

1.54mL

30.75mL

6.15mL

3.08mL

Itanapraced 技术信息

CAS号749269-83-8
分子式C16H11Cl2FO2
分子量 325.162
别名 CHF5074;CSP-1103;CS 1103
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(322.92 mM),配合低频超声助溶,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
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