• 產(chǎn)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

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

• 體外研究：
  Itanapraced (0.03-100 μM) 抑制表達 APPswe 的人神經(jīng)膠質(zhì)瘤細胞 (H4swe) 分泌，對 Aβ42 和 Aβ40 的 IC50 值分別為 3.6 和 18.4 μM。 Itanapraced (5-200 μM) 在濃度大于 15 μM 時，抑制 HEK293swe 細胞的 Notch 加工。 Itanapraced (0-1000 μM; 30 min) 劑量依賴性抑制動作電位，IC50 值為 106 μM。 Itanapraced (30-100 μM) 劑量依賴性地抑制興奮性突觸傳遞。 Itanapraced (1-10 μM) 能顯著降低缺氧葡萄糖 (OGD) 誘導的海馬神經(jīng)元細胞凋亡

• 體內(nèi)研究：
  Itanapraced (口服；375 ppm 加入飲食中，17 周) 在 Tg2576 轉(zhuǎn)基因小鼠降低 Aβ42 和 Aβ40 水平以及腦斑塊負擔。 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.

• 參考文獻：
  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

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

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本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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