Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 692 | 5日内发货 | ||
25 mg | ¥ 5,300 | 8-10周 | ||
50 mg | ¥ 6,890 | 8-10周 | ||
100 mg | ¥ 10,600 | 8-10周 |
Fiboflapon sodium 的其他形式现货产品:
产品描述 | Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood. |
靶点活性 | LTB4:76 nM |
体外活性 | When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon (AM803) inhibited LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon (AM803) dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, AM803 increased survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).Fiboflapon (AM803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog.?Fiboflapon (AM803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model.?Oral administration of Fiboflapon (AM803) (1 mg/kg) resulted in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. |
别名 | GSK2190915 sodium salt, AM-803 sodium |
分子量 | 660.83 |
分子式 | C38H43N3NaO4S |
CAS No. | 1196070-26-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32 mg/mL (48.50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5132 mL | 7.5662 mL | 15.1325 mL | 37.8312 mL |
5 mM | 0.3026 mL | 1.5132 mL | 3.0265 mL | 7.5662 mL | |
10 mM | 0.1513 mL | 0.7566 mL | 1.5132 mL | 3.7831 mL | |
20 mM | 0.0757 mL | 0.3783 mL | 0.7566 mL | 1.8916 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 sodium 1196070-26-4 Immunology/Inflammation LTR GSK2190915 sodium salt GSK2190915 sodium AM-803 sodium Inhibitor inhibitor inhibit