Clofazimine 2030-63-9

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Molecular Weight:

473.4 Clofazimine 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.






Biological Activity


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


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.

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Product Categories : Metabolism > Phospholipase Inhibitor