Chloroquine diphosphate

Catalog No.S4157

For research use only.

Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).

Chloroquine diphosphate Chemical Structure

CAS No. 50-63-5

Selleck's Chloroquine diphosphate has been cited by 172 publications

Purity & Quality Control

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Biological Activity

Description Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Targets
TLR3 [4]
()
TLR7 [4]
()
TLR8 [4]
()
TLR9 [4]
()
ATM [1]
(Cell-free assay)
In vitro

Chloroquine is a chemotherapeutic agent for the clinical treatment of malaria. Chloroquine is able to bind to DNA, and inhibit DNA replication and RNA synthesis which in turn results in cell death. The effect of Chloroquine may also be related to the formation of a toxic heme-Chloroquine complex. Chloroquine inhibits trophozoite hemoglobin degradation through increasing vacuolar pH and inhibiting the activity of vacuolar phospholipase, vacuolar proteases, and heme polymerase[1]. Chloroquine possesses definite antirheumatic properties. Chloroquine has immuno-modulatory effects, suppressing the production/release of tumour necrosis factor and interleukin 6. Moreover, Chloroquine exerts direct antiviral effects, inhibiting pH-dependent steps of the replication of several viruses including members of the flaviviruses, retroviruses, and coronaviruses. Its best-studied effects are those against HIV replication[2]. Chloroquine can accumulate inside the macrophage phagolysosome by ion trapping where it exerts potent antifungal activity against Histoplasma capsulatum and Cryptococcus neoformans by distinct mechanisms. Chloroquine inhibits growth of H. capsulatum by pH-dependent iron deprivation, whereas it is directly toxic to C. neoformans[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human K562 cells MkLpR5l1d3SxeHnjxsBie3OjeR?= NY\JV5huS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;M{GuPFMhdk1? NHLpVoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEWzPFU3Pyd-MUi1N|g2Pjd:L3G+
human KB cells MonRR5l1d3SxeHnjxsBie3OjeR?= NV\BWYJkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JiY3XscJMh[nlibXnjdo9xdGG2ZTDt[ZRpd2RuIFnDOVA:OC54IN88US=> MmXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTR4NEC1NlQoRjF2NkSwOVI1RC:jPh?=
human MDA-MB-468 cells MWnDfZRwfG:6aXRCpIF{e2G7 MWW0PEBp NX7aXZpoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEOuOUB2VSB2LTiyMYNpdG:{bz2xNGgueGinbn;4ZZpqdi1zMD35cEkuViyQLXTp[ZRpgWykdYThck0yNWGvaX7lJIh6\HKxY3jsc5Jq\GVuIFfJOVA:Oi56MTFOwG0> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2NUG5O{c,OTl7NEWxPVc9N2F-
human MCF7 cells NHLPW4hEgXSxdH;4bYPDqGG|c3H5 MWG0PEBp NULwNlZuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJFAvPCC3TTCxMUgyNSh2LTi3MZBp\W67bD2xTE1qdWmmYYrvX|QtPS2pXYH1bY5wgGGuaX6tOk16dCmkZX76fYwqeGmyZYLp[IlvNTRveXypMVFJNWKnborvX4RecW2rZHH6c4wuOih|SDmtc45mNCCJSUWwQVUvPTFizszN NVWxZlJVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFUyQTdpPkG5PVQ2OTl5PD;hQi=>
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human HeLa cells NXLQXmpUS3m2b4TvfIlkyqCjc4PhfS=> Mo\WR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTB;M{Cg{txO M2\pSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W0N|IzLz5{NEO1OFMzOjxxYU6=
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HepG2 MULDfZRwfG:6aXPpeJkh[XO|YYm= M4f4WFczKGi{cx?= MmDRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFMxKM7:TT6= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd2MUGzNUc,OjF5NEGxN|E9N2F-
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HepG2 M4D5SWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWL1R3ZFPzJiaILz NUTGNnFZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCFQ{WwJF0hOzBizszNMi=> NUi3V3RSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPFIzPjdpPkK1NlgzOjZ5PD;hQi=>
HepG2 NXLiS|Z1S3m2b4TvfIlkcXS7IHHzd4F6 M{DRSlczKGi{cx?= MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBESzVyIE2gN|Ah|ryPLh?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh3MkGzNkc,OjF6NUKxN|I9N2F-
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HepG2 NIHBW2VHfW6ldHnvckBie3OjeR?= M2jkVXJm\HWldHnvckBqdiCJRmCg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKHCuYYPtbYR{KGOxLXX4dJJme3OrbnegS2ZRKGGwZDDzbHJPSXNiYXfhbY5{fCCURW[tSXJD[mW2YTDmc4xtd3enZDDifUBkd22yb4Xu[EB1emWjdH3lcpQhOjRiaILzJJBwe3RvdILhcpNn\WO2aX;uJIFv\CCvZXHzeZJm\CB2ODDodpMheG:|dDDkc5Nm MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF|NUS3NUc,OjZzM{W0O|E9N2F-
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Assay
Methods Test Index PMID
Western blot ZEBRA / p-S824 KAP1 ; p62 / LC3 28249048 26677873
Immunofluorescence p-S824 KAP1 / ZEBRA ; CD1d-β2m / LAMP1 ; SQSTM1 / MAP1LC3B 28249048 20368272 29872540
Growth inhibition assay Cell viability 25521075

Protocol (from reference)

Solubility (25°C)

In vitro

Water 100 mg/mL
(193.85 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 515.86
Formula

C18H26ClN3.2H3O4P

CAS No. 50-63-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04443270 Not yet recruiting Drug: Chloroquine phosphate COVID-19 CMN 20 de Noviembre July 27 2020 Phase 1
NCT04462367 Recruiting -- COVID19|Coronavirus Infection|Pregnancy Disease|Severe Acute Respiratory Syndrome Instituto Materno Infantil Prof. Fernando Figueira July 1 2020 --
NCT04340544 Terminated Drug: Hydroxychloroquine|Drug: Placebo COVID-19 University Hospital Tuebingen|Robert Bosch Medical Center|Universitätsklinikum Hamburg-Eppendorf|Bernhard Nocht Institute for Tropical Medicine April 22 2020 Phase 2
NCT04334148 Completed Drug: Hydroxychloroquine|Drug: Placebo oral tablet COVID-19 Adrian Hernandez|Patient-Centered Outcomes Research Institute|Duke University April 22 2020 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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