Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Chloroquine phosphate (Aralen phosphate) 是广泛用于疟疾和类风湿性关节炎的抗疟疾和抗炎剂。它是autophagy 和toll-like receptors 抑制剂,有效抑制SARS-CoV-2(COVID-19) 感染 (EC50=1.13 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 298 | 现货 | ||
100 mg | ¥ 418 | 现货 | ||
200 mg | ¥ 656 | 现货 | ||
500 mg | ¥ 1,270 | 现货 |
产品描述 | Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs). |
靶点活性 | Cytotoxicity against human K562 cells:31.83 nM, Cytotoxicity against hμMan KB cells by microplate method:0.6 μM |
体外活性 | Chloroquine (20 μM)可抑制 IL-12p70 的释放,并降低活化的人单核细胞衍生的朗格汉斯样细胞(MoLC)的 Th1 诱导能力。Chloroquine (20 μM)可增强 IL-1 诱导的 MoLC IL-23 分泌,并随后增加启动的 CD4+ T 细胞的 IL-17A 释放[1]。Chloroquine (25 μM)可抑制亲代 MDA-MB-231 细胞在常氧和缺氧情况下的 MMP-9 mRNA 表达。Chloroquine 对 MMP-2、MMP-9 和 MMP-13 mRNA 的表达具有细胞、剂量和缺氧依赖性影响[2]。使用Chloroquine 抑制 TLR7 和 TLR9 可显著减少体外 HuH7 细胞的增殖[3]。 |
体内活性 | 在正位小鼠模型中,Chloroquine (80 mg/kg,静脉注射)不能阻止 TLR9 表达水平高或低的三阴性 MDA-MB-231 细胞的生长[2]。使用Chloroquine 抑制 TLR7 和 TLR9 可显著抑制小鼠异种移植模型中肿瘤的生长。Chloroquine 也能显著抑制 DEN/NMOR 大鼠模型中 HCC 的发展 [3]。 |
细胞实验 | The cells are cultured in 6-well plates with normal culture medium in the presence of vehicle or 25 or 50 μM chloroquine, until near confluency, after which they are rinsed with sterile phosphate-buffered saline (PBS) and cultured further for the indicated times in serum-free culture medium. At the desired time-points, the culture medium is discarded and the cells are quickly harvested in lysis buffer and clarified by centrifugation. Subsequent to boiling the supernatants in reducing sodium dodecyl sulfate (SDS) sample buffer, equal amounts of protein (100 μg) are loaded per lane and the samples are electrophoresed into 10 or 4-20% gradient polyacrylamide SDS gels, then transferred to a nitrocellulose membrane. To detect TLR9, the blots were incubated overnight at 4°C with anti-TLR9 antibodies, diluted 1:500 in Tris-buffered saline with 0.1% (v/v) Tween-20 (TBST). Equal loading is confirmed with polyclonal rabbit anti-actin. Secondary detection is performed with horseradish peroxidase-linked secondary antibodies. The protein bands are visualized by chemiluminescence using an ECL kit [2]. |
动物实验 | Control and TLR9 siRNA MDA-MB-231 cells (5×105 cells in 100 μL) are inoculated into the mammary fat pads of four-week-old, immune-deficient mice (athymic nude/nu Foxn1). Treatments are started seven days after tumor cell inoculation. The mice are treated daily either with intraperitoneal (i.p.) chloroquine (80 mg/kg) or vehicle (PBS). The animals are monitored daily for clinical signs. Tumor measurements are performed twice a week and tumor volume is calculated according to the formula V=(π/6) (d1×d2)3/2, where d1 and d2 are perpendicular tumor diameters. The tumors are allowed to grow for 22 days, at which point the mice are sacrificed and the tumors are dissected for a final measurement. Throughout the experiments, the animals are maintained under controlled pathogen-free environmental conditions (20-21°C, 30-60% relative humidity and a 12-h lighting cycle). The mice are fed with small-animal food pellets and supplied with sterile water ad libitum [2]. |
别名 | Chloroquine diphosphate, Aralen phosphate, 磷酸氯喹, Chingamin phosphate |
分子量 | 515.87 |
分子式 | C18H26CLN3·2(H3PO4) |
CAS No. | 50-63-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Insoluble
H2O: 10 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 1.9385 mL | 9.6924 mL | 19.3847 mL | 48.4618 mL |
5 mM | 0.3877 mL | 1.9385 mL | 3.8769 mL | 9.6924 mL | |
10 mM | 0.1938 mL | 0.9692 mL | 1.9385 mL | 4.8462 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。
Chloroquine phosphate 50-63-5 Autophagy Immunology/Inflammation Microbiology/Virology Proteases/Proteasome Antibiotic Parasite TLR HIV Protease SARS-CoV inhibit Chingamin Phosphate COVID-19 Chloroquine Inhibitor rheumatoid immune-modulating Toll-like Receptor (TLR) HIV Chloroquine diphosphate Aralen phosphate SARS coronavirus Chloroquine Phosphate infection 磷酸氯喹 Human immunodeficiency virus arthritis Chloroquine Diphosphate malaria inflammatory Chingamin phosphate Aralen Phosphate inhibitor