CAS |
50-63-5 |
Chinese Name |
磷酸氯喹 |
English Name |
Chloroquine Diphosphate |
Synonyms |
Aralen phosphate;Chingamin phosphate |
Molecular Formula |
C18H26ClN3·2H3PO4 |
Molecular Weight |
515.86 |
Solubility |
Soluble in Water ≥60mg/mL |
Purity |
HPLC≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 200-055-2 |
MDL |
MFCD00069852 |
SMILES |
O=P(O)(O)O.O=P(O)(O)O.CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC |
InChIKey |
QKICWELGRMTQCR-UHFFFAOYSA-N |
InChI |
InChI=1S/C18H26ClN3.2H3O4P/c1-4-22(5-2)12-6-7-14(3)21-17-10-11-20-18-13-15(19)8-9-16(17)18;2*1-5(2,3)4/h8-11,13-14H,4-7,12H2,1-3H3,(H,20,21);2*(H3,1,2,3,4) |
PubChem CID |
64927 |
Target Point |
Autophagy;ATM;Toll-like Receptor (TLR) |
Passage |
Autophagy;DNA Damage/DNA Repair; PI3K/Akt/mTOR;Immunology & Inflammation |
Background |
Chloroquine phosphate is an inhibitor of autophagy and Toll-like receptors (TLRs), as well as an ATM activator, and is widely used in researches such as antimalarial and anti-inflammatory drugs for the treatment of malaria and rheumatoid arthritis.According to reports, the drug can effectively inhibit the infection of the novel coronavirus 2019-nCoV that broke out in Wuhan at the cellular level. |
Biological Activity |
Chloroquine diphosphate是一种广泛用于治疗疟疾和类风湿性关节炎的抗疟疾和抗炎药。 Chloroquine 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。[1-3] |
In Vitro |
氯喹(CHQ,20μM)抑制IL-12p70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引发能力。氯喹(CHQ,20μM)增强MoLC中IL-1诱导的IL-23分泌,随后通过引发的CD4 + T细胞增加IL-17A释放[1]。氯喹(25μM)抑制亲本MDA-MB-231细胞中常氧和缺氧中的MMP-9mRNA表达。氯喹对MMP-2,MMP-9和MMP-13 mRNA表达具有细胞,剂量和缺氧依赖性作用[2]。使用IRS-954或氯喹抑制TLR7和TLR9可显著降低体外HuH7细胞的增殖[3]。 |
In Vivo |
氯喹(80 mg/kg,ip)不能阻止原位小鼠模型中具有高或低TLR9表达水平的三阴性MDA-MB-231细胞的生长[2]。使用IRS-954或氯喹的TLR7和TLR9抑制显著抑制小鼠异种移植模型中的肿瘤生长。 DEN/NMOR大鼠模型中的HCC发育也被氯喹显著抑制[3]。 |
Cell Experiment |
将细胞在载体或25或50μM氯喹存在下在具有正常培养基的6孔板中培养,直至接近汇合,之后用无菌磷酸盐缓冲盐水(PBS)冲洗并进一步培养指定的时间。在无血清培养基中。在所需的时间点,弃去培养基并在裂解缓冲液中快速收获细胞并通过离心澄清。在还原十二烷基硫酸钠(SDS)样品缓冲液中煮沸上清液后,每道加载等量的蛋白质(100μg),将样品电泳到10或4-20%梯度聚丙烯酰胺SDS凝胶中,然后转移到硝酸纤维素膜上。膜。为了检测TLR9,将印迹在4℃下与抗TLR9抗体一起温育过夜,在含有0.1%(v/v)Tween-20(TBST)的Tris缓冲盐水中1:500稀释。用多克隆兔抗肌动蛋白确认等量加载。用辣根过氧化物酶连接的二抗进行二次检测。使用ECL试剂盒通过化学发光使蛋白质条带可视化。 |
Animal Experiment |
将对照和TLR9 siRNA MDA-MB-231细胞(100μL中的5×10 5个细胞)接种到4周龄免疫缺陷小鼠(无胸腺裸/ nu Foxn1)的乳房脂肪垫中。在肿瘤细胞接种后7天开始治疗。每天用腹膜内(ip)氯喹(80mg/kg)或载体(PBS)处理小鼠。每天监测动物的临床症状。每周进行两次肿瘤测量,并根据公式V =(π/ 6)(d1×d2)3/2计算肿瘤体积,其中d1和d2是垂直肿瘤直径。使肿瘤生长22天,此时处死小鼠并解剖肿瘤用于最终测量。在整个实验中,将动物维持在受控制的无病原体环境条件下(20-21℃,30-60%相对湿度和12小时光照循环)。给小鼠喂食小动物食物颗粒,随意提供无菌水。 |
Data Literature Source |
[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. |
Unit |
Piece |
Specification |
100mg 10mM*1mL in Water 200mg |