For research use only.
Catalog No.S4107 Synonyms: NSC-141046
CAS No. 2030-63-9
Clofazimine (NSC-141046) is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2.
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|Description||Clofazimine (NSC-141046) is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2.|
|Features||Intracellular activities of Clofazimine are superior to that of B4154.|
Clofazimine stimulates oxygen consumption and superoxide generation by neutrophils, Clofazimine also causes phospholipase A2 activation in neutrophils, resulting in increased release of lysophosphatidylcholine and arachidonic acid from neutrophil membranes. Clofazimine inhibits mitogen-induced stimulation of peripheral blood mononuclear cells. Clofazimine stabilizes lysosomal membranes in macrophages and inhibits Mycobacterium leprae metabolism in mouse peritoneal macrophages.  Clofazimine (5 mg/mL) causes dose-related enhancement of the activity of phospholipase A2 in S. aureus, according to an increase in the release of 3H-radiolabeled arachidonate and lysophosphatidylethanolamine ([3H]LPE) from bacterial-membrane phospholipids.  Clofazimine inhibits 90% of twenty M. tuberculosis strains with MICs <1.0 μg/mL, to be noted, clofazimine inhibits M. tuberculosis strain 2227 with MICs of 0.06 μg/mL. Clofazimine (1 μg/mL) dose-dependently inhibits activity of J774A.1 macrophages. 
|In vivo||Clofazimine (20 mg/kg) prevents mortality and causes a significant reduction in the numbers of CFU in the lungs and spleens of C57BL/6 mice infected M.tuberculosis H37Rv.  Liposomal Clofazimine (L-CLF) (50 mg/kg) dose-dependently reduces CFU 2 to 3 log units in the spleen, liver, and lungs of acutely infected mice with Mycobacterium tuberculosis Erdman.  Clofazimine (500 μg, bid) results in highest Clofazimine concentrations in spleens and livers of mice whereas Clofazimine concentrations in the lungs are significantly lower. Clofazimine (20 mg/kg) is effective in reducing bacterial loads in the liver, spleen and lungs of C57BL/6 mice experimentally infected with M. avium strain TMC 724. |
-  Arbiser JL, et al. J Am Acad Dermatol, 1995, 32(2 Pt 1), 241-247.
-  Van Rensburg CE, et al. Antimicrob Agents Chemother, 1992, 36(12), 2729-2735.
-  Reddy VM, et al. Antimicrob Agents Chemother, 1996, 40(3), 633-636.
|In vitro||DMSO||5 mg/mL (10.56 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04239326||Not yet recruiting||Diagnostic Test: targeted Next Generation Sequencing (tNGS)||Tuberculosis Multidrug-Resistant||Foundation for Innovative New Diagnostics Switzerland||October 2020||--|
|NCT03341767||Terminated||Drug: Clofazimine|Drug: Placebo||Cryptosporidiosis||University of Washington|Bill and Melinda Gates Foundation|The Emmes Company LLC|Calibr a division of Scripps Research|Liverpool School of Tropical Medicine|University of Virginia|Malawi-Liverpool-Wellcome Trust Clinical Research Programme||December 14 2017||Phase 2|
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