Hydroxychloroquine

Name: Hydroxychloroquine
Brand: MedChemExpress
SKU: HY-W031727
Rating: 5.0 (87 reviews)

Cat. No.: HY-W031727 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling.

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

CAS No. : 118-42-3

Size	Stock	Quantity
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
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 87 publication(s) in Google Scholar

Other Forms of Hydroxychloroquine:

Hydroxychloroquine-d₄-1 sulfate In-stock
Hydroxychloroquine sulfate In-stock
Hydroxychloroquine (Standard) In-stock
(S)-Hydroxychloroquine Get quote
(R)-Hydroxychloroquine Get quote
Hydroxychloroquine-d₅ Get quote

87 Publications Citing Use of MCE Hydroxychloroquine

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

Cell Imaging/Staining

In Vivo Efficacy Study

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 31;23(1):243. [Abstract]; The combenefit analysis was performed to identify the synergistic interaction of drug combinations (cDDP + venetoclax, cDDP + HCQ (50-100 μM, 72 h), or cDDP + venetoclax + HCQ (0-50 μM, 72 h)) in H446/cDDP or H196/cDDP cells.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 31;23(1):243. [Abstract]; CCK-8 assay was used to detect the relative cell viability of H446/cDDP under drug combinations (cDDP + venetoclax, cDDP + HCQ (0-50 μM, 0-72 h), or cDDP + venetoclax + HCQ (0-50 μM, 0-72 h)) indicated above.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 31;23(1):243. [Abstract]; The colony formation assay demonstrated and analyzed the effectiveness of HCQ (0-50 μM) within 14 days.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 31;23(1):243. [Abstract]; Western blot analysis showed the expression levels of p62, LC3 I, and LC3 II in H446/cDDP cells after HCQ (0-50 μM, 0-72 h) treatment.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 31;23(1):243. [Abstract]; Combinations of cDDP/VP-16/PTX, venetoclax and HCQ (15 mg/kg, once every two days, ip, 2-3 weeks) shrink the tumor volume of chemoresistant SCLC in PDX mice model.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jun 14;13(1):3419. [Abstract]; Following treatment with the autophagy inhibitor hydroxychloroquine (HCQ, 60 mg/kg, once every other day, ip,18 days), Ursofalk no longer enhanced PD-1 antibody-mediated LLC tumor suppression.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Autophagy. 2023 May;19(5):1533-1550. [Abstract]; 293T cells were transfected with the indicated plasmids above for 8 h and then either treated with Hydroxychloroquine sulfate (CQ; 20 μM) or not. 12 h later, cell lysates were analyzed with western blotting.

: Hydroxychloroquine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3966-3982. [Abstract]; Representative photos of SH-SY5Y xenografted tumors. Mice were intraperitoneally treated with saline (Ctrl), magnolol (35 mg/kg), Hydroxychloroquine sulfate (HCQ; 50 mg/kg), Ac220 (1.5 mg/kg), magnolol þ HCQ, magnolol þ Ac220 for 23 days.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

View All Isoforms

Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms

TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Plasmodium

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	33 μM Compound: HCQ	Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method	[PMID: 25699157]
HCC827	IC₅₀	65 μM Compound: HCQ	Antiproliferative activity against human HCC827 cells after 72 hrs by SRB method Antiproliferative activity against human HCC827 cells after 72 hrs by SRB method	[PMID: 25699157]
NCI-H460	IC₅₀	74 μM Compound: HCQ	Antiproliferative activity against human H460 cells after 72 hrs by SRB method Antiproliferative activity against human H460 cells after 72 hrs by SRB method	[PMID: 25699157]
Vero	CC₅₀	36.9 μM Compound: Hydroxychloroquine	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis	[PMID: 33479570]
Vero C1008	CC₅₀	273.2 μM Compound: HCQ	Cytotoxicity against african green monkey Vero E6 cells by CCK8 assay Cytotoxicity against african green monkey Vero E6 cells by CCK8 assay	[PMID: 33609889]
Vero C1008	CC₅₀	356.4 μM Compound: Hydroxychloroquine	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability	[PMID: 37329713]
Vero C1008	EC₅₀	0.72 μM Compound: 2	Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in viral replication measured upto 48 hrs by qRT-PCR assay Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in viral replication measured upto 48 hrs by qRT-PCR assay	[PMID: 33486200]

In Vitro

Hydroxychloroquine ( 0-100 μM, 48h) can inhibit the activity of SARS-CoV-2 virus in Vero E6 cells^[4].
Hydroxychloroquine has anEC₅₀ value of 1.1-12 μM for various coronaviruses and has low cytotoxicity in various cell lines^[4].
Hydroxychloroquine (0-100 μM, 0-48 hours) inhibits metabolic activity, proliferation and activation of extracellular signal-regulated kinase ERK 1/2 ERK in human dermal fibroblasts (HDFs)^[5].
Hydroxychloroquine (1-100 μM, 12/24 hours) induces a specific type of cell death in human skin fibrocytes (HDFs) that is characterized by surface exposure to phosphatidylserine but is not accompanied by DNA fragmentation^[5].
Hydroxychloroquine induces autophagy in skin fibrocytes (HDFs) by promoting the expression of autophagy regulator Beclin-1 at RNA and protein levels^[5].

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

Western Blot Analysis^[3]

Cell Line:	Human dermal fibroblasts (HDFs)
Concentration:	30 μM
Incubation Time:	0-48 hours
Result:	Time-dependently decreases ERK1/2 phosphonylaf lon at Thr202/Tyr204.

In Vivo

Hydroxychloroquine (HCQ) (25 μM, Intraperitoneal injection (i.p.), Once a week for two weeks) has the effect of reducing the survival rate of endometriosis cells and the number of lesions and histopathology in mouse models of endometriosis^[6].
Hydroxychloroquine has the effect of increasing the number of peritoneal macrophages and the level of IP-10 chemokine in mouse models of endometriosis^[6].
Hydroxychloroquine (3-100 mg/kg, Intraperitoneal injection (i.p.), 1 dose) significantly reduced the size of thrombus and the total time to thrombosis in a mouse model of IgG-APS^[8].
Hydroxychloroquine (10 mg/kg/d, gavage for 5 weeks) can reduce hypertension, endothelial dysfunction and organ damage in mice with severe lupus^[8].

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

Molecular Weight

335.87

Formula

C₁₈H₂₆ClN₃O

CAS No.

118-42-3

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C2C(NC(CCCN(CCO)CC)C)=CC=NC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (297.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1M HCl : 100 mg/mL (297.73 mM; adjust pH to 2 with HCl)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9773 mL	14.8867 mL	29.7734 mL
5 mM	0.5955 mL	2.9773 mL	5.9547 mL
10 mM	0.2977 mL	1.4887 mL	2.9773 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% Corn Oil
Solubility: ≥ 5 mg/mL (14.89 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 5 mg/mL (14.89 mM); Clear solution
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.89 mM); Clear solution

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).

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: 99.82%

Select Batch:

Data Sheet (276 KB) SDS (597 KB)

COA (243 KB) HNMR (270 KB) RP-HPLC (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Manzo C, et al. Psychomotor Agitation Following Treatment with Hydroxychloroquine. Drug Saf Case Rep. 2017 Dec;4(1):6. [Content Brief]

[2]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40. [Content Brief]

[3]. Yao X, et al. In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Clin Infect Dis. 2020 Mar 9. pii: ciaa237. [Content Brief]

[4]. Persoons L, et al. Broad spectrum anti-coronavirus activity of a series of anti-malaria quinoline analogues. Antiviral Res. 2021;193:105127. [Content Brief]

[5]. Ramser B, et al. Hydroxychloroquine modulates metabolic activity and proliferation and induces autophagic cell death of human dermal fibroblasts. J Invest Dermatol. 2009;129(10):2419-2426. [Content Brief]

[6]. Ruiz A, et al. Effect of hydroxychloroquine and characterization of autophagy in a mouse model of endometriosis. Cell Death Dis. 2016;7(1):e2059. Published 2016 Jan 14. [Content Brief]

[7]. Edwards MH, et al. Hydroxychloroquine reverses thrombogenic properties of antiphospholipid antibodies in mice. Circulation. 1997;96(12):4380-4384. [Content Brief]

[8]. Gómez-Guzmán M, et al. Chronic hydroxychloroquine improves endothelial dysfunction and protects kidney in a mouse model of systemic lupus erythematosus. Hypertension. 2014;64(2):330-337. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / 1M HCl	1 mM	2.9773 mL	14.8867 mL	29.7734 mL	74.4336 mL
	5 mM	0.5955 mL	2.9773 mL	5.9547 mL	14.8867 mL
	10 mM	0.2977 mL	1.4887 mL	2.9773 mL	7.4434 mL
	15 mM	0.1985 mL	0.9924 mL	1.9849 mL	4.9622 mL
	20 mM	0.1489 mL	0.7443 mL	1.4887 mL	3.7217 mL
	25 mM	0.1191 mL	0.5955 mL	1.1909 mL	2.9773 mL
	30 mM	0.0992 mL	0.4962 mL	0.9924 mL	2.4811 mL
	40 mM	0.0744 mL	0.3722 mL	0.7443 mL	1.8608 mL
	50 mM	0.0595 mL	0.2977 mL	0.5955 mL	1.4887 mL
	60 mM	0.0496 mL	0.2481 mL	0.4962 mL	1.2406 mL
	80 mM	0.0372 mL	0.1861 mL	0.3722 mL	0.9304 mL
	100 mM	0.0298 mL	0.1489 mL	0.2977 mL	0.7443 mL