Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Edicotinib (JNJ-527) 是能够透过血脑屏障的、口服具有活性的、选择性的CSF-1R 抑制剂 (IC50:3.2 nM)。它对 KIT (IC50:20 nM) 和 FLT3 (IC50:190 nM) 的抑制作用较小。它抑制小胶质细胞的扩张,减弱小胶质细胞的增殖和神经退行性变。它可用于研究阿尔茨海默病和类风湿性关节炎。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 463 | 现货 | ||
2 mg | ¥ 679 | 现货 | ||
5 mg | ¥ 1,120 | 现货 | ||
10 mg | ¥ 1,530 | 现货 | ||
25 mg | ¥ 3,280 | 现货 | ||
50 mg | ¥ 4,780 | 现货 | ||
100 mg | ¥ 6,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,170 | 现货 |
产品描述 | Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment. |
靶点活性 | FLT3:190 nM, Kit:20 nM , CSF-1R:3.2 nM |
体外活性 | Edicotinib (0.1 nM-1μM; 24 hours) causes a dose-dependent decrease of CSF1R activation. Edicotinib (0.1 nM-1μM; 24 hours) lead to a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose-response curve displays the effect of Edicotinib on CSF1R and ERK1/2 (IC50: 18.6 nM and 22.5 nM for CSF1R and ERK1/2) [1]. |
体内活性 | Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced, however not other inflammatory cytokines. Edicotinib (oral gavage; 3, 10, 30, and 100 mg/kg; 5 days) obviously inhibits microglial proliferation in ME7 mice.?It reduces the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg. At every dose tested (CD45+CD11b high Ly6C intermediate/low cells), JNJ-527 depletes up to 50% of patrolling blood monocytes. Only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high?cells) at 100 mg/kg [1]. Edicotinib displays a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively [1]. |
别名 | JNJ-527, JNJ-40346527 |
分子量 | 461.6 |
分子式 | C27H35N5O2 |
CAS No. | 1142363-52-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15 mg/mL (32.4 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 | 2.1664 mL | 10.8319 mL | 21.6638 mL | 54.1594 mL |
5 mM | 0.4333 mL | 2.1664 mL | 4.3328 mL | 10.8319 mL | |
10 mM | 0.2166 mL | 1.0832 mL | 2.1664 mL | 5.4159 mL | |
20 mM | 0.1083 mL | 0.5416 mL | 1.0832 mL | 2.708 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。
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