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Clofazimine

Name: Clofazimine
Brand: Selleck Chemicals
SKU: S4107
Rating: 5 (4 reviews)

Catalog No.S4107 Synonyms: NSC-141046

For research use only.

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.

CAS No. 2030-63-9

Selleck's Clofazimine has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description

Features

Intracellular activities of Clofazimine are superior to that of B4154.

Targets

PLA2 ^[1]

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

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]

Protocol (from reference)

References

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Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	473.4
Formula	C₂₇H₂₂Cl₂N₄
CAS No.	2030-63-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl

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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05294146	Recruiting	Drug: Clofazimine	Nontuberculous Mycobacterial Diseases	Radboud University Medical Center	February 14 2022	Phase 2
NCT04239326	Recruiting	Diagnostic Test: targeted Next Generation Sequencing (tNGS)	Tuberculosis Multidrug-Resistant	Foundation for Innovative New Diagnostics Switzerland	April 16 2021	--
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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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