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> Hydroxychloroquine (sulfate) [747-36-4]

Hydroxychloroquine (sulfate) [747-36-4]

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Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

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Hydroxychloroquine sulfate Chemical Structure

Hydroxychloroquine sulfate Chemical Structure

CAS No. : 747-36-4

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

Based on 56 publication(s) in Google Scholar

Other Forms of Hydroxychloroquine sulfate:

  • (S)-Hydroxychloroquine Obtenir un devis
  • (R)-Hydroxychloroquine Obtenir un devis
  • Hydroxychloroquine-d4 sulfate Obtenir un devis
  • Hydroxychloroquine Obtenir un devis
  • Hydroxychloroquine sulfate (Standard) Obtenir un devis

Voir tous les produits spécifiques à Isoform Parasite:

Voir toutes les isoformes
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR):

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6
Description

Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro[1][2][3].

IC50 & Target

TLR7

 

Plasmodium

 

TLR9

 

Cellular Effect
Cell Line Type Value Description References
Vero C1008 CC50
> 40 μM
Compound: Hydroxychloroquine sulfate
Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)
Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)
10.1101/2020.04.03.023846
Vero C1008 CC50
>> 50 μM
Compound: Hydroxychloroquine Sulfate
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
>> 50 μM
Compound: Hydroxychloroquine Sulfate
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
11.17 μM
Compound: Hydroxychloroquine Sulfate
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 EC50
4.17 μM
Compound: Hydroxychloroquine sulfate
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
10.1101/2020.04.03.023846
Vero C1008 IC50
9.21 μM
Compound: Hydroxychloroquine Sulfate
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
In Vitro

Hydroxychloroquine sulfate is a synthetic antimalarial drug derived from 4-aminoquinoline; it has been used for several decades for the treatment of some rheumatic diseases such as rheumatoid arthritis (RA)[1]. Five micromolar Hydroxychloroquine sulfate or chloroquine also has no measurable effect on intracellular pH, although these concentrations can inhibit TLR9 or 7 signaling induced by DNA or RNA ligands[2].

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

Hydroxychloroquine sulfate Related Antibodies
In Vivo

Hydroxychloroquine sulfate is prescribed for the treatment of lupus, and both Hydroxychloroquine sulfate and its analog chloroquine inhibit TLR7 and 9 signaling[2].

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

433.95

Formule

C18H28ClN3O5S
CAS No.

747-36-4
Appearance

Solid

Color

White to off-white

SMILES

CCN(CCO)CCCC(NC1=CC=NC2=CC(Cl)=CC=C12)C.O=S(O)(O)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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)

Solvant et solubilité
In Vitro: 

H2O : 110 mg/mL (253.49 mM; Need ultrasonic and warming)

DMSO : 100 mg/mL (230.44 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 2.3044 mL 11.5221 mL 23.0441 mL
5 mM 0.4609 mL 2.3044 mL 4.6088 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.

* 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.

  • Calculateur de molarité

  • Calculateur de dilution

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (230.44 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Pureté et documentation

Purity: 99.99%

SDS (394 KB)

COA (246 KB) HNMR (188 KB) LCMS (404 KB)

Instruction de manipulation (2659 KB)
Références

  • [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]

Administration animale
[2]

MRL/lpr mice are dosed orally five times a week with 20 or 60 mg/kg E6446 or 60 mg/kg Hydroxychloroquine sulfate beginning at 5 weeks of age. CB 4564 is administered at 50 mg/kg i.p. every 10 days. A serum sample is taken immediately before the beginning of treatment to monitor changes in autoreactive antibodies. Subsequently, serum samples are collected approximately monthly and analyzed for anti-dsDNA by ELISA after 1:500 dilution. Body weights and urine samples are taken at the same interval, and proteinuria is assessed. Anti-nuclear antibodies (ANA) are assessed using commercially available HEp2 slide kits, with serum diluted to 1:100 in kit buffer. ANA scores are read blinded[2].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références

  • [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]

  • [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.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.3044 mL 11.5221 mL 23.0441 mL 57.6103 mL
5 mM 0.4609 mL 2.3044 mL 4.6088 mL 11.5221 mL
10 mM 0.2304 mL 1.1522 mL 2.3044 mL 5.7610 mL
15 mM 0.1536 mL 0.7681 mL 1.5363 mL 3.8407 mL
20 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8805 mL
25 mM 0.0922 mL 0.4609 mL 0.9218 mL 2.3044 mL
30 mM 0.0768 mL 0.3841 mL 0.7681 mL 1.9203 mL
40 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
50 mM 0.0461 mL 0.2304 mL 0.4609 mL 1.1522 mL
60 mM 0.0384 mL 0.1920 mL 0.3841 mL 0.9602 mL
80 mM 0.0288 mL 0.1440 mL 0.2881 mL 0.7201 mL
100 mM 0.0230 mL 0.1152 mL 0.2304 mL 0.5761 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 sulfate Related Classifications

  • Anti-infection Immunology/Inflammation Autophagy
  • Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy
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Keywords:

Hydroxychloroquine747-36-4HCQParasiteToll-like Receptor (TLR)SARS-CoVAutophagySARS coronavirusInhibitorinhibitorinhibit