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MedChemExpressModel 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[1][2][3].
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Hydroxychloroquine sulfate

MCE China:Hydroxychloroquine sulfate

Brand:MedChemExpress (MCE)

Cat. No.HY-B1370

CAS:747-36-4

Synonyms:HCQ sulfate

Purity:99.95%

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)

Shipping:Room temperature in continental US; may vary elsewhere.

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.

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].

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].

Animal Administration: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].

IC50 & Target:TLR7 Plasmodium TLR9

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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]

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