盐酸氟西汀杂质
- CAS号:3545-67-3
- 英文名:N4-(7-chloro-4-quinolyl)-N1,N1-diethylpentane-1,4-diamine dihydrochloride
- 中文名:盐酸氟西汀杂质
- CBNumber:CB3929733
- 分子式:C18H28Cl3N3
- 分子量:392.79402
- MOL File:3545-67-3.mol
盐酸氟西汀杂质性质、用途与生产工艺
- 生物活性 Chloroquine dihydrochloride 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 dihydrochloride 是autophagy 和toll-like receptors (TLRs) 的抑制剂。Chloroquine dihydrochloride 有效抑制 SARS-CoV-2 (COVID-19) 感染 (EC50=1.13 μM)。
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靶点
HIV-1
Malaria
TLRs
SARS-COV-2
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体外研究
Chloroquine dihydrochloride (20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine dihydrochloride (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells[1]. Chloroquine dihydrochloride (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine dihydrochloride 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 dihydrochloride significantly reduces HuH7 cell proliferation in vitro.
Chloroquine dihydrochloride (0.01-100 μM; 48 hours) potently blocked virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC50=1.13 μM). Chloroquine dihydrochloride 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. -
体内研究
Chloroquine dihydrochloride (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 dihydrochloride 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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