产品
编 号:F250234
分子式:C27H22Cl2N4
分子量:473.4
产品类型
结构图
CAS No: 2030-63-9
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产品详情
生物活性:
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research.
体内研究:
Clofazimine (100,50 mg/kg, 口服, 每日一次, 14 d) 对小鼠内的结核分枝杆菌具有延迟性抗菌活性。Animal Model:Female BALB/c mice (age 6–8 weeks, mass 18–20 g)
Dosage:100, 50, 25, 12.5, 6.25, 3.125 or 1.5625 mg/kg
Administration:Oral gavage (p.o.), once per day for 14 d
Result:Exhibited an increase of the lung bacterial load during the first 7 days of treatment, and decreased the CFU counts in the lungs of mice after 10 days of treatment. Significantly declined the lung CFU counts in 100 or 50 mg/ kg group at 14th day.
体外研究:
Clofazimine (0.0625-2 mg/L, 14 d) 在前 2-4 天的处理中对结核分歧杆菌无明显活性,在 1 周后表现出浓度依赖性的抗菌活性:在浓度为或低于 0.25 mg/L (MIC) 时具有抑菌活性、在浓度高于 MIC 时具有杀菌活性。以异烟肼为阳性对照。Clofazimine (10 μM, 24 h) 抑制血液肿瘤细胞 (Jurkat、U266、Namalwa、K562、HL60) 的生长。Clofazimine (1-50 μM, 12-48 h) 对 U266 细胞的抑制作用呈剂量和时间依赖性。Clofazimine (10 μM, 24-48 h) 可使 U266 细胞线粒体膜去极化,显著增加 caspase-3 激活水平 (25倍),并增加早期和晚期凋亡细胞的百分比。