Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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50g |
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Other Sizes |
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Purity: ≥98%
Chloroquine phosphate is reported to be highly effective in combating SARS-CoV-2 (COVID-19, CoronaVirus, or the COVID-19 pandemic) infection in vitro. It functions as a strong inhibitor of autophagy and toll-like receptors (TLRs) and a 4-aminoquinoline antimalarial drug that is used to treat and prevent malaria in regions where the disease is known to be susceptible to its effects. In addition to being an ATM activator, it also has anti-rheumatoid properties. Chloroquine diphosphate has been documented as an adjuvant for chemotherapy and radiation therapy to induce autophagy in cells and prevent the proliferation or metastasis of anti-cancer cells. The process by which chloroquine diphosphate induces autophagy in cells involves arresting them in the G1 phase, which up-regulates the expression of p53 and p27 and down-regulates the expression of CDK2 and cyclin D1.
Targets |
Plasmodium; Malaria; TLRs; SARS-COV-2; HIV-1
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Chloroquine suppressed matrix metalloproteinase (MMP)-2 and MMP-9 mRNA expression and protein activity, whereas MMP-13 mRNA expression and proteolytic activity were increased. Despite enhancing TLR9 mRNA expression, chloroquine suppressed TLR9 protein expression in vitro.[2]
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Cell Assay |
The cells are cultivated in 6-well plates using normal culture medium with either vehicle or 25 or 50 μM chloroquine until they are almost confluent. Afterward, they are rinsed with sterile phosphate-buffered saline (PBS) and continue to culture in serum-free culture medium for the specified durations. Centrifugation is used to quickly harvest the cells in lysis buffer and clarify them after the culture medium is discarded at the predetermined time points. Once the supernatants have been boiled in reducing sodium dodecyl sulphate (SDS) sample buffer, 100 μg of protein is loaded into each lane. The samples are then electrophoresed into 10 or 4–20% gradient polyacrylamide SDS gels before being placed onto a nitrocellulose membrane. TLR9 is detected by incubating the blots with anti-TLR9 antibodies diluted 1:500 in Tris-buffered saline containing 0.1% (v/v) Tween-20 (TBST) for an overnight period at 4°C. Polyclonal rabbit anti-actin is used to confirm equal loading. Horseradish peroxidase-linked secondary antibodies are used in secondary detection. Using an ECL kit, the protein bands can be seen through chemiluminescence.
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Animal Protocol |
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References |
Molecular Formula |
C18H32CLN3O8P2
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Molecular Weight |
515.86
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Exact Mass |
515.14
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Elemental Analysis |
C, 41.91; H, 6.25; Cl, 6.87; N, 8.15; O, 24.81; P, 12.01
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CAS # |
50-63-5
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Related CAS # |
Chloroquine phosphate;50-63-5;Chloroquine-d5;1854126-41-2;Chloroquine dihydrochloride;3545-67-3;Chloroquine-d5 diphosphate; 132-73-0 (sulfate); 1854126-42-3; 54-05-7 ;151-69-9 (acetate) ; 1446-17-9 (phosphate); 3545-67-3 (HCl) ; 50-63-5 (diphosphate) ;
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PubChem CID |
64927
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Appearance |
White to light yellow crystalline powder
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Boiling Point |
460.6ºC at 760 mmHg
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Melting Point |
200 °C
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Flash Point |
232.3ºC
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LogP |
3.03
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tPSA |
203.3
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SMILES |
CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O
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InChi Key |
QKICWELGRMTQCR-UHFFFAOYSA-N
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InChi Code |
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)
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Chemical Name |
4-N-(7-chloroquinolin-4-yl)-1-N,1-N-diethylpentane-1,4-diamine;phosphoric acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (193.85 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03529396 | Active Recruiting |
Drug: Chloroquine Drug: Primaquine |
Vivax Malaria G6PD Deficiency |
Fundação de Medicina Tropical Dr. Heitor Vieira Dourado |
July 20, 2018 | Phase 2 |
NCT02932007 | Active Recruiting |
Drug: Chloroquine Phosphate | Atrial Fibrillation | University of South Florida | March 28, 2017 | Phase 2 |
NCT06076837 | Not yet recruiting | Drug: Chloroquine Phosphate Drug: Balstilimab |
Pancreatic Cancer Metastatic | HonorHealth Research Institute | December 2023 | Phase 1 |
NCT05443178 | Recruiting | Drug: Nivaquine ® (Chloroquine) | Tuberculosis Infection | University of Zurich | January 4, 2022 | Phase 1 |
NCT04704999 | Not yet recruiting | Drug: Chloroquine Drug: Tafenoquine |
Plasmodium Vivax Malaria | University of Oxford | September 18, 2023 | Phase 4 |
Tumour volume reduced with chloroquine and IRS-954. Intrahepatic and extrahepatic tumours (black and red arrows respectively) derived from (a) HuH7 and (b) HepG2 cells injected into NOD-SCID mouse livers. Liver Int . 2015 Mar;35(3):1063-76. td> |
Reduced TLR7, Akt, p-Akt & NF-кB expression with chloroquine in rat HCCs. Liver Int . 2015 Mar;35(3):1063-76. td> |
Zymograms of supernatants from vehicle, 25 or 50 μM chloroquine-treated parental MDA-MB-231 cells or control siRNA or TLR9 siRNA cells after 24 h of treatment in normoxia (N) or hypoxia (H). Oncol Lett . 2013 Dec;6(6):1665-1672. td> |