1. Autophagy
    Immunology/Inflammation
    Anti-infection
  2. Parasite
    Autophagy
    SARS-CoV
    Toll-like Receptor (TLR)
    HIV
  3. Chloroquine phosphate

Chloroquine phosphate 

目录号: HY-17589 纯度: 99.89%
产品使用指南

Chloroquine phosphate 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剂。Chloroquine phosphate 是 autophagytoll-like receptors (TLRs) 的抑制剂。Chloroquine phosphate 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 Chemical Structure

CAS No. : 50-63-5

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Customer Review

Other Forms of Chloroquine phosphate:

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

    Chloroquine phosphate purchased from MCE. Usage Cited in: Tumour Biol. 2016 Jul;37(7):8811-24.

    Assays for autophagy activity. Immunoblot analysis for LC3B. Compared with the Lenti-NC cells, the Lenti-CD44v6 cells display a higher intensity of autophagy flux but not steady-state levels when treated with 5-FU (*P<0.001).

    Chloroquine phosphate purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.

    p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80 μM ω-3 FFAs, 20 μM ATRA alone or in combination for 48 h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2016 Dec;48(12):1075-1084.

    The change of LC3 is analyzed by western blotting after 6 h hypoxia in the presence or absence of Chloroquine of WDR26-overexpressing H9c2 cells.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    Cells are treated with RA (20 μM) plus ω-3 PUFAs (80 μM) with or without CQ (5 μM) for 24 h. Cell extracts are prepared and subjected to western blotting analysis.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.

    L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Oncogene. 2018 May;37(22):2936-2952.

    IPZ-treated U87 and U251 cells are treated with or without Baf-A1 (5 nM), CQ (40 μM), or MG132 (1 μM) for 48 h, followed by western blots.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):501-507.

    Western blot analysis of autophagy markers and LAMP2 in mice with AAV-vaspin and Chloroquine (CQ) pretreatment after I/R (1d).

    Chloroquine phosphate purchased from MCE. Usage Cited in: Neurosci Lett. 2018 Aug 24;682:112-117.

    After treatment of CDDP with or without the autophagy inhibitor CQ, the expression of LC3-II in the CQ+CDDP group is less than that in the CQ group but is higher than that in the CDDP group at 24 h and 96 h.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Chloroquine phosphate purchased from MCE. Usage Cited in: J Pharmacol Exp Ther. 2018 Oct;367(1):20-27.

    Protein expression of LC3B and p62 in Panc-1 cells treated with Carboxamidotriazole (CAI) and/or Chloroquine (CQ).

    Chloroquine phosphate purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Dec;109:1617-1627.

    GFP-LC3B-expressing LX-2 cells are treated with DMSO, 3-MA (10 mM), or Chloroquine (30 μM) alone or in the presence of Carvedilol (CVD, 10 μM) for 24 h. The conversion of LC3B-I to LC3B-II is evaluated using immunoblotting.

    Chloroquine phosphate purchased from MCE. Usage Cited in: EBioMedicine. 2017 May;19:49-59.

    mCherry-GFPLC3 puncta analysis in SPC-A-1 cells. Cells are transfected with mCherry-GFP-LC3 plasmid and incubated for 6 h. Next, cells are pretreated with or without Chloroquine (50 μM) for 1 h followed by stimulation of 5 μM Flu for 24 h or 36 h. Scale bar, 10 μm and 2 μm (magnified graph). The lysosomal inhibitor Chloroquine (CQ) raises the lysosomal pH and increases the autophagic flux.

    Chloroquine phosphate purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.

    MC3T3-E1 cells are treated with AICAR (10 μM) in the presence or absence of 3-MA (5 mM) or CQ (10 μM) for 24 h, after which western blot analysis is conducted.
    • 生物活性

    • 实验参考方法

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    • 参考文献

    Description

    Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is a autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].

    IC50 & Target

    TLRs, HIV, SARS-COV-2, Autophagy[1][2][3][4]

    In Vitro

    Chloroquine (CHQ, 20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (CHQ, 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 IRS-954 or chloroquine significantly reduces HuH7 cell proliferation in vitro[3].
    Chloroquine (0.01-100μM; 48 hours) potently blocks virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC50= 1.13 μM). Chloroquine blocks virus infection by increasing endosomal pH required for virus/cell fusion, as well as interfering with the glycosylation of cellular receptors of SARS-CoV[4].

    In Vivo

    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 IRS-954 or chloroquine significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine[3].

    Clinical Trial
    Molecular Weight

    515.86

    Formula

    C₁₈H₃₂ClN₃O₈P₂

    CAS No.

    50-63-5

    SMILES

    O=P(O)(O)O.O=P(O)(O)O.CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 33 mg/mL (63.97 mM)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9385 mL 9.6926 mL 19.3851 mL
    5 mM 0.3877 mL 1.9385 mL 3.8770 mL
    10 mM 0.1939 mL 0.9693 mL 1.9385 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    References
    Cell Assay
    [2]

    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 sulphate (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 are 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.89%

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    Keywords:

    ChloroquineParasiteAutophagySARS-CoVToll-like Receptor (TLR)HIVSARS coronavirusHuman immunodeficiency virusmalariainflammatoryrheumatoidarthritisSARS-CoV-2COVID-19infectionimmune-modulatingInhibitorinhibitorinhibit

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    产品名称:
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    目录号:
    HY-17589
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