Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂,可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂,在完整的人和诱导的大鼠多形核白细胞 PMNLs 中,其IC50值分别为 3.1 nM 和 6.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
2 mg | ¥ 543 | 现货 | ||
5 mg | ¥ 787 | 现货 | ||
10 mg | ¥ 1,090 | 现货 | ||
25 mg | ¥ 2,380 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 现货 |
产品描述 | Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively). |
靶点活性 | FLAP:1.6 nM |
体外活性 | Quiflapon is an effective inhibitor of leukotriene (LT) biosynthesis in the human, squirrel monkey, and rat whole blood (IC50: 510, 69, and 9 nM, respectively). Quiflapon has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC50 value of 1.6 nM in a FLAP binding assay and inhibition of the photoaffinity labeling of FLAP by two different photoaffinity ligands. However, Quiflapon has no effect on rat 5-lipoxygenase. The inhibition of activation of 5-lipoxygenase was shown through inhibition of the translocation of the enzyme from the cytosol to the membrane in human PMNLs[1]. |
体内活性 | Pups were treated with either vehicle or Quiflapon(10, 20, or 40 mg/kg; daily for days 1-4, 5-9, or 10-14) subcutaneously. On day 14, the lungs were inflated, fixed, and stained for histopathological and morphometric analyses. Inhibition of antigen-induced bronchoconstriction by Quiflapon is observed in inbred rats pretreated with methysergide, Ascaris-challenged squirrel monkeys, and Ascaris-challenged sheep (early and late phase response) [1]. Hyperoxia groups treated with Quiflapon untreated hyperoxia groups displayed definite evidence of aberrant alveolarization but no inflammation[2]. |
别名 | 喹夫拉朋, MK-591 |
分子量 | 587.17 |
分子式 | C34H35ClN2O3S |
CAS No. | 136668-42-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: ≥ 50 mg/mL (85.15 mM)
H2O: < 0.1 mg/mL (insoluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7031 mL | 8.5154 mL | 17.0308 mL | 42.5771 mL |
5 mM | 0.3406 mL | 1.7031 mL | 3.4062 mL | 8.5154 mL | |
10 mM | 0.1703 mL | 0.8515 mL | 1.7031 mL | 4.2577 mL | |
20 mM | 0.0852 mL | 0.4258 mL | 0.8515 mL | 2.1289 mL | |
50 mM | 0.0341 mL | 0.1703 mL | 0.3406 mL | 0.8515 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Quiflapon 136668-42-3 Apoptosis Immunology/Inflammation FLAP MK591 inhibit 5-LO activating protein MK 591 Inhibitor 喹夫拉朋 MK-591 inhibitor