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Chloroquine phosphate

CAS No. : 50-63-5

MCE 国际站：Chloroquine phosphate

产品活性：Chloroquine phosphate 是一种广泛用于疟疾和类风湿性关节炎的抗疟疾和抗炎剂。Chloroquine phosphate 是 autophagy 和 toll-like receptors (TLRs) 的抑制剂。Chloroquine phosphate 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC₅₀=1.13 μM)。

研究领域：Autophagy  |  Immunology/Inflammation  |  Anti-infection

作用靶点：Parasite  |  Autophagy  |  SARS-CoV  |  Toll-like Receptor (TLR)  |  HIV  |  Antibiotic

In Vitro: Chloroquine (CHQ, 20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (CHQ, 20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4⁺ T cells. Chloroquine (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine has cell-, dose- and hypoxia-dependent effects on MMP-2, MMP-9 and MMP-13 mRNA expression. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly reduces HuH7 cell proliferation in vitro.
Chloroquine (0.01-100 μM; 48 hours) potently blocks virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC₅₀= 1.13 μM). Chloroquine blocks virus infection by increasing endosomal pH required for virus/cell fusion, as well as interfering with the glycosylation of cellular receptors of SARS-CoV.

In Vivo: Chloroquine (80 mg/kg, i.p.) does not prevent the growth of the triple-negative MDA-MB-231 cells with high or low TLR9 expression levels in the orthotopic mouse model. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine.

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