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Hydroxychloroquine

MCE China：Hydroxychloroquine

Brand：MedChemExpress (MCE)

Cat. No.HY-W031727

CAS：118-42-3

Purity：99.77%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

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

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.

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].

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].

IC50 & Target：Plasmodium

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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]

[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]