Hydroxychloroquine sulfate(Synonyms: 硫酸羟氯喹; HCQ sulfate)

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Hydroxychloroquine sulfate (Synonyms: 硫酸羟氯喹; HCQ sulfate) 纯度: 99.82%

Hydroxychloroquine sulfate (HCQ sulfate) 是一种合成的抗疟疾剂，也可以抑制 Toll 样受体 7/9 (TLR7/9) 信号传导。Hydroxychloroquine sulfate 有效抑制 SARS-CoV-2 感染。

Hydroxychloroquine sulfate(Synonyms: 硫酸羟氯喹; HCQ sulfate)

Hydroxychloroquine sulfate Chemical Structure

CAS No. : 747-36-4

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生物活性

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

Antimalarial[1], TLR7/9[2]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

433.95

Formula

C18H28ClN3O5S
CAS 号

747-36-4
中文名称

硫酸羟氯喹；硫酸羟基氯喹
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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)
溶解性数据
In Vitro: 

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

DMF : 1.4 mg/mL (3.23 mM; Need ultrasonic)

DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 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
10 mM 0.2304 mL 1.1522 mL 2.3044 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： PBS

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

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [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.
Animal Administration
[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 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.