Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fiboflapon (GSK2190915) 是一种可口服且具有有效性 5-脂氧合酶激活蛋白 (FLAP) 抑制剂,结合 FLAP 的效价为 2.9 nM,对人血中 LTB4 有抑制作用, IC50 值为 76 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 419 | 现货 | ||
2 mg | ¥ 591 | 现货 | ||
5 mg | ¥ 987 | 现货 | ||
10 mg | ¥ 1,630 | 现货 | ||
25 mg | ¥ 3,570 | 现货 | ||
50 mg | ¥ 6,890 | 现货 | ||
100 mg | ¥ 9,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,430 | 现货 |
产品描述 | Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM. |
靶点活性 | LTB4:76 nM |
体外活性 | Fiboflapon (AM-803) demonstrates excellent preclinical toxicology and pharmacokinetics in both rats and dogs. In the rodent bronchoalveolar lavage (BAL) model, Fiboflapon (AM-803) also exhibits prolonged pharmacological effects[2]. |
体内活性 | Orally administered at 1 mg/kg, Fiboflapon (AM-803) sustains a continuous inhibition of ex vivo ionophore-stimulated whole blood leukotriene B4 (LTB4) biosynthesis, with an inhibition rate exceeding 90% for up to 12 hours, and an EC50 of approximately 7 nM. When rat lungs are subjected to in vivo calcium ionophore challenge, Fiboflapon (AM-803) inhibits the production of LTB4 and cysteinyl leukotrienes (CysLT) with ED50 values of 0.12 mg/kg and 0.37 mg/kg, respectively. Following a single oral dose of 3 mg/kg, the inhibition rates measured 16 hours later for LTB4 and CysLT are 86% and 41%, respectively. In an acute inflammatory environment, Fiboflapon dose-dependently reduces LTB4, CysLT, plasma protein extravasation, and neutrophil influx induced by intraperitoneal yeast glucan injection. Lastly, Fiboflapon increases the survival time of mice exposed to intravenous injection of lethal platelet-activating factor (PAF) [2]. |
别名 | GSK2190915, AM-803 |
分子量 | 637.83 |
分子式 | C38H43N3O4S |
CAS No. | 936350-00-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40 mg/mL (62.71 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5678 mL | 7.8391 mL | 15.6782 mL | 39.1954 mL |
5 mM | 0.3136 mL | 1.5678 mL | 3.1356 mL | 7.8391 mL | |
10 mM | 0.1568 mL | 0.7839 mL | 1.5678 mL | 3.9195 mL | |
20 mM | 0.0784 mL | 0.392 mL | 0.7839 mL | 1.9598 mL | |
50 mM | 0.0314 mL | 0.1568 mL | 0.3136 mL | 0.7839 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。
Fiboflapon 936350-00-4 Immunology/Inflammation FLAP AM 803 GSK2190915 AM-803 GSK-2190915 GSK 2190915 AM803 Inhibitor inhibitor inhibit