Hydroxychloroquine Sulfate (Synonyms: HCQ, NSC 4375) |
Katalog-Nr.GC12544
One-Click Copy Product Info
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Autophagie-Inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 747-36-4
Sample solution is provided at 25 µL, 10mM.
Hydroxychloroquine Sulfate is a synthetic 4-aminoquinoline derivative that serves as an antimalarial drug. Hydroxychloroquine Sulfate exerts its antimalarial effect by targeting the heme metabolism pathway in Plasmodium, disrupting the polymerization of toxic heme and ultimately causing parasite death[1]. Beyond antimalarial activity, Hydroxychloroquine Sulfate is widely in the research of autoimmune diseases (e.g., rheumatoid arthritis[2], systemic lupus erythematosus[3]), as well as cancer and COVID-19[4][5].
In vitro, treatment of SARS-CoV-2-infected Vero cells with chloroquine or Hydroxychloroquine Sulfate (0.032–100μM) for 24–48 hours decreased the viral replication in a concentration-dependent manner, and Hydroxychloroquine Sulfate(EC50=0.72μM) was found to be more potent than chloroquine (EC50=5.47μM)[6]. Pretreatment of RAW 264.7 cells with 5μM Hydroxychloroquine Sulfate for 2h potently inhibited CpG2006 DNA-induced NF-κB activation (IC50=1.2μM, >95% suppression) and showed superior selectivity for nucleic acid ligands (EC50=1.4μM for RNA40) over small-molecule agonist R-848 (EC50 >10μM)[7].
In vivo, Hydroxychloroquine Sulfate (60mg/kg; oral; 5 times/week for 7 weeks) significantly reduced serum anti-dsDNA antibody titers by 40% (p<0.05 vs. control) in MRL/lpr mice, but had no significant effect on proteinuria or survival.Pretreatment with Hydroxychloroquine Sulfate (20mg/kg; oral; 18 h) reversed CpG1668-induced serum IL-6 elevation by >60%[7].
References:
[1] Caminal-Montero, L., & Suárez-Díaz, S. (2019). Hydroxychloroquine and Antimalarials. The Journal of rheumatology, 46(11), 1547.
[2] Schrezenmeier, E., & Dörner, T. (2020). Mechanisms of action of hydroxychloroquine and chloroquine: implications for rheumatology. Nature reviews. Rheumatology, 16(3), 155–166.
[3] Ponticelli, C., & Moroni, G. (2017). Hydroxychloroquine in systemic lupus erythematosus (SLE). Expert opinion on drug safety, 16(3), 411–419.
[4] Ferreira, P. M. P., Sousa, R. W. R., Ferreira, J. R. O., Militão, G. C. G., & Bezerra, D. P. (2021). Chloroquine and hydroxychloroquine in antitumor therapies based on autophagy-related mechanisms. Pharmacological research, 168, 105582.
[5] Sinha, N., & Balayla, G. (2020). Hydroxychloroquine and COVID-19. Postgraduate medical journal, 96(1139), 550–555.
[6] Yao, X., Ye, F., Zhang, M., Cui, C., Huang, B., Niu, P., Liu, X., Zhao, L., Dong, E., Song, C., Zhan, S., Lu, R., Li, H., Tan, W., & Liu, D. (2020). 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). Clinical infectious diseases : an official publication of the Infectious Diseases Society of America, 71(15), 732–739.
[7] Lamphier, M., Zheng, W., Latz, E., Spyvee, M., Hansen, H., Rose, J., Genest, M., Yang, H., Shaffer, C., Zhao, Y., Shen, Y., Liu, C., Liu, D., Mempel, T. R., Rowbottom, C., Chow, J., Twine, N. C., Yu, M., Gusovsky, F., & Ishizaka, S. T. (2014). Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo.
| Cell experiment [1]: | |
Cell lines | Vero cells |
Preparation Method | The Vero cells were derived from the African green monkey kidney and were grown in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 5% fetal bovine serum. Cells were seeded into 96-well plates at a density of 1×104cells/well and were grown for 24 hours. The in vitro experiment was divided into two sections, named: (i) the treatment study and (ii) the prophylactic study. Treatment study: In the treatment study Vero cells were infected at a multiplicity of infection (MOI) of 0.01 (100PFU/well) for 2 hours at a temperature of 37°C. Virus input was washed with DMEM and the cells were then treated with medium containing either chloroquine or Hydroxychloroquine Sulfate at 0.032, 0.16, 0.80, 4, 20, 100μM for 24 or 48 hours. The supernatant was collected, and, the RNA was extracted and analyzed by relative quantification using RT-PCR. |
Reaction Conditions | 0.032, 0.16, 0.80, 4, 20, 100μM; 24 or 48h |
Applications | Hydroxychloroquine Sulfate decreased the viral replication in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | MRL/lpr mice |
Preparation Method | MRL/lpr mice were dosed orally five times a week with 20mg/kg or 60mg/kg E6446 or 60mg/kg Hydroxychloroquine Sulfate beginning at 5 weeks of age for 7 weeks. Cytoxan was administered at 50mg/kg i.p. every 10 days. A serum sample was taken immediately before the beginning of treatment to monitor changes in autoreactive antibodies. Subsequently serum samples were collected approximately monthly and analyzed for anti-dsDNA by ELISA after 1:500 dilution Body weights and urine samples were taken at the same interval, and proteinuria assessed by ChemStrips. Anti-nuclear antibodies (ANA) were assessed using commercially available HEp2 slide kits, with serum diluted to 1:100 in kit buffer. ANA scores were read blinded. |
Dosage form | 60mg/kg; p.o.; 5 times/week for 7 weeks |
Applications | Hydroxychloroquine Sulfate significantly reduced serum anti-dsDNA antibody titers by 40%. |
References: | |
| Cas No. | 747-36-4 | SDF | |
| Überlieferungen | HCQ, NSC 4375 | ||
| Chemical Name | 2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethanol;sulfuric acid | ||
| Canonical SMILES | CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O | ||
| Formula | C18H28ClN3O5S | M.Wt | 433.95 |
| Löslichkeit | ≥ 17.6mg/mL in Water | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3044 mL | 11.5221 mL | 23.0441 mL |
| 5 mM | 460.9 μL | 2.3044 mL | 4.6088 mL |
| 10 mM | 230.4 μL | 1.1522 mL | 2.3044 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)