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• 产品描述： Quiflapon sodium (MK591) is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP).

• 靶点： FLAP

• 体内研究：
  Hyperoxia groups of mice treated with Quiflapon sodium (20, 40 mg/kg) show alveolarization that resembles that of room air controls while untreated hyperoxia groups show definite evidence of aberrant alveolarization but no inflammation. A comparison of the Aβ-immunopositive areas between the placebo and Quiflapon sodium (320 mg/kg)-treated group reveals a statistically significant reduction of the amyloid burden in the treated mice. Quiflapon sodium also has a significant reduction in brain levels of IL-1β. Mice treated with Quiflapon sodium show a statistically significant decrease in the steady-state levels of total CREB and its phosphorylated form at Ser133

• 细胞实验： LNCaP cells (appr 3×10^5) are plated and treated with inhibitors or solvent vehicle for varying periods of time. Then the cells are lysed in lysis buffer containing 0.2% CHAPS detergent plus protease and phosphatase inhibitors, and the enzymatic activity of Akt is measured by a kit following methods supplied by the manufacturer.

• 动物实验： The Tg2576 transgenic mice expressing human APP with the Swedish mutation (K670N/M671L) are used. They are genotyped by PCR analysis using tail DNA and kept in a pathogen-free environment, on a 12-hour light/dark cycle and have access to food and water ad libitum. All the experiments presented in this paper are performed with female mice. Starting at 7 months of age, mice are randomized to receive MK-591 (40 mg/kg weight) (n=11) or vehicle (n=9) in their chow diet for 8 months until they are 15 months old. Considering that each mouse eats on average 5 g/day of chow diet and the diet is formulated for 320 mg Quiflapon sodium per kg diet, the final dose of the active drug is approximately 40 mg/kg weight/day. During the study, mice in both groups gained weight regularly, and no significant difference in weight is detected between the two groups. No macroscopic effect on the overall general health is observed in the animals receiving active treatment. Post-mortem examination shows no sign of macroscopic patholog

• 参考文献：
  1. Sarveswaran S, et al. MK591, a leukotriene biosynthesis inhibitor, induces apoptosis in prostate cancer cells: synergistic action with LY294002, an inhibitor of phosphatidylinositol 3'-kinase. Cancer Lett. 2010 May 28;291(2):167-76. 2. Park MS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitor MK-0591 prevents aberrant alveolarization in newborn mice exposed to 85% oxygen in a dose- and time-dependent manner. Lung. 2011 Feb;189(1):43-50. 3. Mendis C, et al. Effect of 5-lipoxygenase inhibitor MK591 on early molecular and signaling events induced by staphylococcal enterotoxin B in human peripheral blood mononuclear cells. FEBS J. 2008 Jun;275(12):3088-98. 4. Chu J, et al. Involvement of 5-lipoxygenase activating protein in the amyloidotic phenotype of an Alzheimer's disease mouse model. J Neuroinflammation. 2012 Jun 14;9:127.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.642 ml	8.208 ml	16.416 ml
  5 mM	0.328 ml	1.642 ml	3.283 ml
  10 mM	0.164 ml	0.821 ml	1.642 ml
  50 mM	0.033 ml	0.164 ml	0.328 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 *