| 名称 | Clofazimine |
| 描述 | Clofazimine (NSC-141046) is a phenazine dye with anti-mycobacterial and anti-inflammatory activities. Clofazimine has a slow bactericidal effect on Mycobacterium leprae and is active against various other Mycobacteria. |
| 体外活性 | Administered bi-daily at 500 μg, Clofazimine accumulates at the highest concentrations in the spleen and liver, while significantly reduced levels are observed in the lungs. A dosage of 20 mg/kg of Clofazimine can prevent death by significantly decreasing the colony-forming unit (CFU) count in the lungs and spleen of C57BL/6 mice infected with the tuberculosis bacillus Mycobacterium tuberculosis H37Rv. The same dosage effectively lowers bacterial numbers in the liver, spleen, and lungs of C57BL/6 mice infected with the Mycobacterium avium strain TMC724. Moreover, 50 mg/kg of Liposomal Clofazimine in acute infection reduces CFUs in the spleen, liver, and lungs of mice harboring the Erdman strain of tuberculosis, exhibiting dose-dependency. |
| 体内活性 | At a concentration of 1 μg/mL, Clofazimine inhibits the activity of J774A.1 macrophages in a dose-dependent manner. The compound targets neutrophils, activating phospholipase A2 which, in turn, increases the release of lysophosphatidylcholine and arachidonic acid from the neutrophil membrane. In macrophages, Clofazimine stabilizes lysosomal membranes and impedes the metabolism of Mycobacterium leprae within murine peritoneal macrophages. Additionally, Clofazimine exhibits a 90% inhibition rate on 20 strains of Mycobacterium tuberculosis with minimum inhibitory concentrations (MICs) of less than 1.0 μg/mL. It also suppresses the mitogen-induced proliferation of peripheral blood mononuclear cells. |
| 存储条件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 1 mg/mL, Sonication is recommended.
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| 关键字 | Clofazimine | NSC 141046 | Inhibitor | NSC141046 | Bacterial | Antibiotic | inhibit |
| 相关产品 | Neomycin sulfate | Ampicillin sodium | Kanamycin sulfate | Sulfamethoxazole sodium | Doxycycline | Dimethyl sulfoxide |
| 相关库 | 经典已知活性库 | 抗癌临床化合物库 | 抗病毒库 | 药物功能重定位化合物库 | FDA 上市药物库 | 抗癌上市药物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌药物库 |
United States
