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Chloroquine phosphate

Chloroquine phosphate

产品编号 T0194   CAS 50-63-5
别名: Chloroquine diphosphate, Aralen phosphate, 磷酸氯喹, Chingamin phosphate

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)。

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Chloroquine phosphate Chemical Structure
Chloroquine phosphate, CAS 50-63-5
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
其他形式的 Chloroquine phosphate:
产品目录号及名称: Chloroquine phosphate (T0194)
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纯度: 99.79%
纯度: 99.68%
纯度: 99.64%
纯度: 98%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
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 by MTT assay:31.83 nM, Cytotoxicity against hμMan KB cells by microplate method:0.6 μM
体外活性 Chloroquine (20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells [1]. Chloroquine (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine has cell-, dose- and hypoxia-dependent effects on MMP-2, MMP-9 and MMP-13 mRNA expression [2]. TLR7 and TLR9 inhibition using chloroquine significantly reduce HuH7 cell proliferation in vitro [3].
体内活性 Chloroquine (80 mg/kg, i.p.) does not prevent the growth of the triple-negative MDA-MB-231 cells with high or low TLR9 expression levels in the orthotopic mouse model [2]. TLR7 and TLR9 inhibition using chloroquine significantly inhibit tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine [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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: Insoluble

H2O: 10 mM

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Said A, et al. Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells. J Immunol. 2014 Dec 15;193(12):6135-43. 2. Tuomela J, et al. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672. 3. Mohamed FE, et al. Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2014 Jul 2. doi: 10.1111/liv.12626. 4. Su Q, Wang J, Liu F, et al. Blocking Parkin/PINK1-mediated mitophagy sensitizes hepatocellular carcinoma cells to sanguinarine-induced mitochondrial apoptosis[J]. Toxicology in Vitro. 2020: 104840. 6. Hanyu X, Lanyue L, Miao D, et al. Effect of Ganoderma applanatum polysaccharides on MAPK/ERK pathway affecting autophagy in breast cancer MCF-7 cells[J]. International Journal of Biological Macromolecules. 2020, 146: 353-362 7. Zhou Y, Wang Y, Wu S, et al. Sulforaphane-cysteine inhibited migration and invasion via enhancing mitophagosome fusion to lysosome in human glioblastoma cells[J]. Cell Death & Disease. 2020, 11(9): 1-16. 8. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530.

文献引用

1. Liu X, Xi H, Han S, et al.Zearalenone induces oxidative stress and autophagy in goat Sertoli cells.Ecotoxicology and Environmental Safety.2023, 252: 114571. 2. Guo S, Xu Z, Feng Q, et al.Molecular mechanism by which RRM2-inhibitor (cholagogue osalmid) plus bafilomycin A1 cause autophagic cell death in multiple myeloma.Archives of Biochemistry and Biophysics.2023: 109771. 3. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 4. Zhou Y, Wang Y, Wu S, et al. Sulforaphane-cysteine inhibited migration and invasion via enhancing mitophagosome fusion to lysosome in human glioblastoma cells. Cell Death & Disease. 2020, 11(9): 1-16. 5. Hanyu X, Lanyue L, Miao D, et al. Effect of Ganoderma applanatum polysaccharides on MAPK/ERK pathway affecting autophagy in breast cancer MCF-7 cells. International Journal of Biological Macromolecules. 2020, 146: 353-362 6. Wang Y, Ji L, Peng Z, et al. Silencing DAPK3 blocks the autophagosome-lysosome fusion by mediating SNAP29 in trophoblast cells under high glucose treatment. Molecular and Cellular Endocrinology. 2020, 502: 110674 7. Su Q, Wang J, Liu F, et al. Blocking Parkin/PINK1-mediated mitophagy sensitizes hepatocellular carcinoma cells to sanguinarine-induced mitochondrial apoptosis. Toxicology in Vitro. 2020: 104840 8. Xi H, Hu Z, Han S, et al. FSH-inhibited autophagy protects against oxidative stress in goat Sertoli cells through p62-Nrf2 pathway. Theriogenology. 2022 9. Su Q, Wu Q, Chen K, et al. Induction of Estrogen Receptor β-mediated Autophagy Sensitizes Breast Cancer Cells to TAD1822-7, a Novel Biphenyl Urea Taspine Derivative. Molecular Biology Reports. 2021 10. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530.
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相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌上市药物库 抗寄生虫库 抗寄生虫天然产物库 天然产物库 免疫/炎症分子化合物库 抗癌天然产物库 抗衰老化合物库 抑制剂库 植物来源化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

Chloroquine phosphate 50-63-5 Autophagy Immunology/Inflammation Microbiology/Virology Proteases/Proteasome SARS-CoV TLR HIV Protease Antibiotic Parasite 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

 

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