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> Hydroxychloroquine [118-42-3]

Hydroxychloroquine [118-42-3]

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Cat# HY-W031727-100mg

Size : 100mg

Brand : MedChemExpress

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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.

Hydroxychloroquine Chemical Structure

Hydroxychloroquine Chemical Structure

CAS No. : 118-42-3

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

Based on 49 publication(s) in Google Scholar

Other Forms of Hydroxychloroquine:

  • Hydroxychloroquine sulfate In-stock
  • Hydroxychloroquine-d4-1 sulfate Get quote
  • Hydroxychloroquine-d5 Get quote

View All Parasite Isoform Specific Products:

View All Isoforms

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

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Description

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[1][2][3][4][5][6][7][8].

IC50 & Target

Plasmodium

 

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.

Hydroxychloroquine Related Antibodies

Cell Line:
Concentration:
Incubation Time:
Result:

Western Blot Analysis[5]

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

Animal Model:
Dosage:
Administration:
Result:
Clinical Trial
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)

H2O : 1.67 mg/mL (4.97 mM; ultrasonic and warming and heat to 60°C)

*"≥" 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
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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 5 mg/mL (14.89 mM); Clear solution

  • Protocol 2

    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)

g

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: ≥98.0%

COA (243 KB) HNMR (127 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]

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

    [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.

    [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.

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

    [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.

    [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.

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

    [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.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO / 1M HCl 1 mM 2.9773 mL 14.8867 mL 29.7734 mL 74.4336 mL
DMSO / 1M HCl 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Hydroxychloroquine Related Classifications

Help & FAQs

Keywords:

Hydroxychloroquine118-42-3ParasiteToll-like Receptor (TLR)SARS-CoVAutophagySARS coronavirusSystemic lupus erythematosusantimalarial agentscutaneous lupuslupus flareslupus nephritisretinopathy.Inhibitorinhibitorinhibit

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