Home Metabolism Dyes inhibitor - Phospholipase (e.g. PLA) activator - Antineoplastic and Immunosuppressive Antibiotics Clofazimine For research use only.

Clofazimine

Synonyms: NSC-141046

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.

Clofazimine Chemical Structure

Clofazimine Chemical Structure

CAS No. 2030-63-9

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Clofazimine Related Products

Biological Activity

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.
Targets
PLA2 [1]
In vitro
In vitro 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. [1] 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. [2] 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. [3]
In Vivo
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. [3] 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. [4] 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. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05294146 Completed
Nontuberculous Mycobacterial Diseases
Radboud University Medical Center
 February 14 2022 Phase 2
NCT04239326 Completed
Tuberculosis Multidrug-Resistant
Foundation for Innovative New Diagnostics Switzerland
 April 16 2021 --
NCT03341767 Terminated
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

Chemical Information & Solubility

Molecular Weight 473.4 Formula

C27H22Cl2N4
CAS No. 2030-63-9 SDF --
Smiles CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (10.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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