Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FIPI (5-Fluoro-2-indolyl deschlorohalopemide) 是 halopemide 的衍生物,抑制PLD1和PLD2,IC50值分别为 25 nM 和 20 nM。它防止 PLD 调节 F-肌动蛋白细胞骨架重组、细胞扩散和趋化性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 282 | 现货 | ||
2 mg | ¥ 398 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,760 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,570 | 现货 | ||
500 mg | ¥ 9,520 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 735 | 现货 |
产品描述 | FIPI (5-Fluoro-2-indolyl deschlorohalopemide) is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. |
靶点活性 | PLD1:25 nM, PLD2:20 nM |
体外活性 | FIPI is a potent, concentration-dependent PLD2 inhibitor, and we show here that it inhibits PLD1 equally well under standard in vitro assay conditions. FIPI was added into the cell culture media 1 h before performing an in vivo PLD assay and was found to be a potent inhibitor of PLD2 with an IC50 of 10 nM.? The typical localization of PLD1 to peri-nuclear membrane vesicles and PLD2 to the plasma membrane were not affected by exposure to FIPI and and FIPI did not decrease PIP2 availability on the plasma membrane in PLD1- and PLD2-overexpressing cells as assessed using an enhanced GFP-fused PIP2 sensor. FIPI did not significantly inhibit p38 or ERK phosphorylation in bone marrow-derived macrophages stimulated with lipopolysaccharide. FIPI inhibition of PLD did diminish fMLP-directed chemotaxis(p < 0.01), validating this role for PLD function and suggesting that PLD regulates chemotaxis via mechanisms distinct from affecting MAKP signaling. |
激酶实验 | Phospholipase D activity is quantified using our established method of measuring the formation of [32P]-radiolabeled PBt. Cellular lipids are extracted and PBt is isolated using our published methods of lipid extraction and thin layer chromatographic separation, respectively. Radioactivity is measured using liquid scintillation counting and quantified as DPM normalized to 106 counts in the total cellular lipid extract or as percentage of control (vehicle-treated cells). |
细胞实验 | Cytotoxicity in MAECs is determined by assaying the extent of reduction in MTT in intact cells using the commercial MTT reduction assay kit. At the end of the experimental treatments, MTT solution (10% vol/vol in MEM) is added and the cells are incubated for 3 hours, following which MTT solvent is added in an amount equal to the original culture volume. Absorbance of the reduced MTT is determined spectrophotometrically, according to the manufacturer's recommendations. |
别名 | 5-Fluoro-2-indolyl deschlorohalopemide |
分子量 | 421.47 |
分子式 | C23H24FN5O2 |
CAS No. | 939055-18-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.5 mg/mL (29.66 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3726 mL | 11.8632 mL | 23.7265 mL | 59.3162 mL |
5 mM | 0.4745 mL | 2.3726 mL | 4.7453 mL | 11.8632 mL | |
10 mM | 0.2373 mL | 1.1863 mL | 2.3726 mL | 5.9316 mL | |
20 mM | 0.1186 mL | 0.5932 mL | 1.1863 mL | 2.9658 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。
FIPI 939055-18-2 Autophagy Metabolism Phospholipase Inhibitor inhibit 5-Fluoro-2-indolyl deschlorohalopemide inhibitor