• 产品描述： Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease

• 靶点： IC50 value: 3.6 μM (Aβ42), 18.4 μM (Aβ40);BetaAmyloid;Gamma-secretase

• 体外研究：
  Itanapraced (0.03-100 μM) 抑制表达 APPswe 的人神经胶质瘤细胞 (H4swe) 分泌，对 Aβ42 和 Aβ40 的 IC50 值分别为 3.6 和 18.4 μM。 Itanapraced (5-200 μM) 在浓度大于 15 μM 时，抑制 HEK293swe 细胞的 Notch 加工。 Itanapraced (0-1000 μM; 30 min) 剂量依赖性抑制动作电位，IC50 值为 106 μM。 Itanapraced (30-100 μM) 剂量依赖性地抑制兴奋性突触传递。 Itanapraced (1-10 μM) 能显著降低缺氧葡萄糖 (OGD) 诱导的海马神经元细胞凋亡

• 体内研究：
  Itanapraced (口服；375 ppm 加入饮食中，17 周) 在 Tg2576 转基因小鼠降低 Aβ42 和 Aβ40 水平以及脑斑块负担。 Animal Model: Male and female Tg2576 transgenic mice expressing Swedish mutated form of human APP (APPswe) Dosage: 375 ppm Administration: Oral administration; 375 ppm in the diet for 17 weeks Result: Reduced total brain Aβ42 and Aβ40 levels, and brain plaque burden in aged Tg2576 mice. Caused no COX-mediated toxic effects in the gastrointestinal tract and Notch-mediated cell differentiation abnormalities in the ileum.

• 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.

• 溶解性： soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.075 ml	15.377 ml	30.754 ml
  5 mM	0.615 ml	3.075 ml	6.151 ml
  10 mM	0.308 ml	1.538 ml	3.075 ml
  50 mM	0.062 ml	0.308 ml	0.615 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *