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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:
药物设计专题培训
千万补贴 助力科研
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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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: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

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

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TargetMol Library Books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.

TargetMol Library Books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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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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