Chloroquine dihydrochloride

Name: Chloroquine dihydrochloride
Brand: MedChemExpress
SKU: HY-17589B
Rating: 5.0 (894 reviews)

Cat. No.: HY-17589B Purity: 99.61%: Data Sheet
COA

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

For research use only. We do not sell to patients.

Chloroquine dihydrochloride Chemical Structure

CAS No. : 3545-67-3

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 894 publication(s) in Google Scholar

Other Forms of Chloroquine dihydrochloride:

Chloroquine-d₅ In-stock
Chloroquine phosphate In-stock
Chloroquine In-stock
Chloroquine-d₅ diphosphate Get quote
Chloroquine-d₄ phosphate Get quote
Chloroquine dihydrochloride (Standard) Get quote

876 Publications Citing Use of MCE Chloroquine dihydrochloride

Cell Viability Assay

Proliferation Assay

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Apr 29;23(1):86. [Abstract]; 293 cells transfected with the indicated vectors were treated with chloroquine (20 μM) or DMSO for 6 h. Cell lysates were prepared, and the CDC6 protein level was measured by Western blotting.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Aug 28. [Abstract]; Chloroquine (50 nM, 24 h), as an autophagy inhibitor, blocks autophagosomal-lysosomal fusion in HT22 cells, leading to impaired autophagic flux.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Jan 22. [Abstract]; The protein levels of SOX2 in 100 μg/mL of PS-NP-exposed Swan 71 cells treated with CHX (10 μg/mL; 4 h) and MG132 (10 μM; 6 h) or chloroquine (CQ) (15 μM; 6 h).

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2024 Jul;13(7):e12468. [Abstract]; Western blotting showing the protein degradation of HEXB by using Chloroquine (CQ) (10 μM, 24 h).

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Res. 2023 Jul 17. [Abstract]; A375 cells were pretreated with CQ (30μM) or MG132 (100 nM) for 2 hours, and then treated with CCCP/FeSO4 plus mannose for 24 hours. Tubulin was used to determine the amount of loading proteins.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2023 Apr 2. [Abstract]; WB analysis of LC3 and p62 expression in MCF7 and SKBR3 cells after YAP1 transient overexpression for 48 h with or without EBSS (6 h) starvation or CQ (Chloroquine) (20 µmol/L, 6 h) treatment.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2023 Nov 15. [Abstract]; Sorafenib-sensitive HepG2 cells, with or without URB1-AS1 overexpression, were treated with the lysosomal inhibitor chloroquine or vehicle for 24 h. Ferritin H levels were analyzed by Western blot.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2023 Jul;12(7):e12342. [Abstract]; After pretreating cells with 10μM CQ, the levels of phospho‐AMPKα and autophagic markers in the cells were quantified by immunoblotting using the specific antibodies. β‐actin serves as a loading control.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2023 Jul;12(7):e12342. [Abstract]; The sEV cocultured 22Rv1 cells were pretreated with 1μM CQ and followed by IR treatment. The cell survival rate was determined using colony survival assay (n = 3).

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Immun Inflamm Dis. 2023 Apr 12; 11:e830.; Chloroquine (10 μM; 30 min) reverses the effect of OmpA on autophagy by inhibiting the expression of Beclin1 and LC3II/I while increasing the expression of P62 in BMDCs.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Immun Inflamm Dis. 2023 Apr 12; 11:e830.; Chloroquine (10 μM; 30 min) reverses the effect of OmpA on autophagy by inhibiting the expression of LC3 in BMDCs.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Jan;79(1):44-53. [Abstract]; Treatment with sub-dose of Everolimus (10 nM), together with CQ (5 µM) increases the levels of Bax and cleaved PARP, and decreases the levels of Bcl-2 expression in both PC3 and LNPER cells.

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Dec;109:1617-1627. [Abstract]; 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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 May;37(22):2936-2952. [Abstract]; 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 dihydrochloride purchased from MedChemExpress. Usage Cited in: J Pharmacol Exp Ther. 2018 Oct;367(1):20-27. [Abstract]; Protein expression of LC3B and p62 in Panc-1 cells treated with Carboxamidotriazole (CAI) and/or Chloroquine (CQ).

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):501-507. [Abstract]; Western blot analysis of autophagy markers and LAMP2 in mice with AAV-vaspin and Chloroquine (CQ) pretreatment after I/R (1d).

: Chloroquine dihydrochloride purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2017 May;19:49-59. [Abstract]; 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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2016 Dec;48(12):1075-1084. [Abstract]; 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2][3]^[5]

Plasmodium

Malaria

TLRs

SARS-COV-2

HIV-1

In Vitro

Chloroquine dihydrochloride (20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine dihydrochloride (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells[1]. Chloroquine dihydrochloride (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine dihydrochloride 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 dihydrochloride significantly reduces HuH7 cell proliferation in vitro^[3].
Chloroquine dihydrochloride (0.01-100 μM; 48 hours) potently blocked virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC50=1.13 μM). Chloroquine dihydrochloride 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].

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

In Vivo

Chloroquine dihydrochloride (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 dihydrochloride significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by Chloroquine^[3].

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

Clinical Trial

Molecular Weight

392.79

Formula

C₁₈H₂₈Cl₃N₃

CAS No.

3545-67-3

Appearance

Solid

Color

White to yellow

SMILES

CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 140 mg/mL (356.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5459 mL	12.7294 mL	25.4589 mL
5 mM	0.5092 mL	2.5459 mL	5.0918 mL
10 mM	0.2546 mL	1.2729 mL	2.5459 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.5 mg/mL (8.91 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.5 mg/mL (8.91 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3.5 mg/mL (8.91 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (245 KB) HNMR (166 KB) RP-HPLC (259 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Colson P, et al. Chloroquine and hydroxychloroquine as available weapons to fight COVID-19. Int J Antimicrob Agents. 2020;55(4):105932. [Content Brief]

[5]. Savarino A, et al. The anti-HIV-1 activity of chloroquine. J Clin Virol. 2001;20(3):131-135. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5459 mL	12.7294 mL	25.4589 mL	63.6472 mL
	5 mM	0.5092 mL	2.5459 mL	5.0918 mL	12.7294 mL
	10 mM	0.2546 mL	1.2729 mL	2.5459 mL	6.3647 mL
	15 mM	0.1697 mL	0.8486 mL	1.6973 mL	4.2431 mL
	20 mM	0.1273 mL	0.6365 mL	1.2729 mL	3.1824 mL
	25 mM	0.1018 mL	0.5092 mL	1.0184 mL	2.5459 mL
	30 mM	0.0849 mL	0.4243 mL	0.8486 mL	2.1216 mL
	40 mM	0.0636 mL	0.3182 mL	0.6365 mL	1.5912 mL
	50 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2729 mL
	60 mM	0.0424 mL	0.2122 mL	0.4243 mL	1.0608 mL
	80 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7956 mL
	100 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6365 mL