产品
编 号:F341027
分子式:C21H26Cl2O
分子量:365.34
产品类型
结构图
CAS No: 37693-01-9
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产品详情
生物活性:
Clofoctol is a bacteriostatic antibiotic. Clofoctol is used in the treatment of respiratory tract and ear, nose and throat infections caused by Gram-positive bacteria. Clofoctol is only functional against Gram-positive bacteria and can penetrate into human lung tissue. Clofoctol is also an inhibitor of prostate cancer. Clofoctol has antiviral potency.
体内研究:
Clofoctol (175 mg/kg;腹腔注射;每日一次,持续 37 天) 能够在人类前列腺癌异种移植小鼠模型中阻断肿瘤生长而没有明显毒性。Clofoctol (62.5 mg/kg;腹腔注射;两次) 抑制 SARS-CoV-2 复制并降低 SARS-CoV-2 感染小鼠的肺部炎症。Animal Model:Male athymic nude mice (BALB/c, nu/nu-NCr) aged 4–6 weeks, human prostate cancer xenograft model
Dosage:175 mg/kg
Administration:Intraperitoneal injection, daily for 37 days
Result:Significantly inhibited PC3 tumour growth, tumour weight was also reduced by 60%.
Animal Model:K18-hACE2 transgenic C57BL/6J mice with SARS-CoV-2 infection
Dosage:62.5 mg/kg
Administration:Intraperitoneal injection, 1h and 8h post-infection
Result:Induced body weight loss, reduced the viral load in the lungs. The expression of transcripts encoding IL-6, TNFα, IL12p40, IFNβ, IFNγ and the interferon-stimulated genes (ISG) Mx1, Ifi44 and ISG15 was markedly reduced.
Animal Model:8–10 week-old female C57BL/6J mice
Dosage:62.5mg/kg
Administration:Intraperitoneal injection, once (Pharmacokinetics)
Result:Reached concentrations up to 61 μM in the lungs and remained above this level for almost 4h as early as 30 min after injection.
体外研究:
Clofoctol (0-100 μM;72 h) 抑制前列腺癌细胞生长。 Clofoctol (0 -20 μM;24 h) 在 G1 阶段。 Clofoctol (0-30 μM;0-24 小时) 诱导 ER 应激并激活 UPR 通路。 Clofoctol (0-40 μM;24 h) 抑制翻译。 Clofoctol (0-100 μM;24 h) 对 SARS-CoV-2 具有抗病毒作用在 Vero-81 和 Vero-81-TMPRSS2 细胞中,IC50 分别为 9.3 μM 和 11.59 μM。