Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2578215A 是一种有效的选择性 LRRK2 激酶抑制剂,对野生型 LRRK2 和 G2019S 突变型的IC50值都约为 10 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 439 | 现货 | ||
10 mg | ¥ 628 | 现货 | ||
50 mg | ¥ 2,311 | 现货 | ||
100 mg | ¥ 3,649 | 现货 | ||
200 mg | ¥ 4,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 439 | 现货 |
产品描述 | GSK2578215A is a potent and selective LRRK2 kinase inhibitor. |
靶点活性 | LRRK2 (WT):10.9 nM, LRRK2 (G2019S):8.9 nM |
体外活性 | 100 mg/kg i.p. GSK2578215A抑制小鼠脾脏和肾中Ser910 和Ser935磷酸化,但在大脑中没有作用. |
体内活性 | SH-SY5Y细胞中,GSK2578215A通过改变自噬体 - 溶酶体融合来损害自噬流,并且通过诱导Drp-1介导的线粒体分裂和线粒体衍生的ROS信号传导诱导线粒体自噬。GSK2578215A在稳定转染到HEK293细胞中的野生型LRRK2和LRRK2 [G2019S]中诱导对Ser910和Ser935磷酸化的剂量依赖性抑制,并诱导小鼠Swiss 3T3细胞中内源性LRRK2的类似的剂量依赖性Ser910和Ser935去磷酸化。 |
激酶实验 | PFV integration assay: For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5′-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5′-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(?) target DNA, 125 mM NaCl, 5 mM MgSO4, 4 μM ZnCl2, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane–HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37 °C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37 °C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5′-CTACTTACTCTAGCTTCCCGGCAAC, 5′-TTCGCCAGTTAATAGTTTGCGCAAC, and 5′-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95 °C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95 °C, 30 seconds annealing at 56 °C and 1 minutes extension at 68 °C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI. |
别名 | 5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰胺 |
分子量 | 399.42 |
分子式 | C24H18FN3O2 |
CAS No. | 1285515-21-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 39.9 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5036 mL | 12.5182 mL | 25.0363 mL | 62.5908 mL |
5 mM | 0.5007 mL | 2.5036 mL | 5.0073 mL | 12.5182 mL | |
10 mM | 0.2504 mL | 1.2518 mL | 2.5036 mL | 6.2591 mL | |
20 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1295 mL | |
50 mM | 0.0501 mL | 0.2504 mL | 0.5007 mL | 1.2518 mL | |
100 mM | 0.025 mL | 0.1252 mL | 0.2504 mL | 0.6259 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。
GSK2578215A 1285515-21-0 Autophagy Mitophagy LRRK2 Mitochondrial Autophagy Inhibitor GSK-2578215A inhibit 5-(2-氟-4-吡啶基)-2-(苯基甲氧基)-N-3-吡啶基苯甲酰胺 Leucine-rich repeat kinase 2 inhibitor