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Clofazimine Dyes inhibitor

Cat.No.S4107

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 of this compound include intercalation of this chemical with bacterial DNA and increasing levels of cellular phospholipase A2.
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Quality Control

Batch: Purity: 99.53%
99.53

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (10.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 473.4 Formula

C27H22Cl2N4

Storage (From the date of receipt)
CAS No. 2030-63-9 -- Storage of Stock Solutions

Synonyms NSC-141046 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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Mechanism of Action

Features
Intracellular activities of Clofazimine are superior to that of B4154.
Targets/IC50/Ki
PLA2
In vitro
Clofazimine stimulates oxygen consumption and superoxide generation by neutrophils, this compound also causes phospholipase A2 activation in neutrophils, resulting in increased release of lysophosphatidylcholine and arachidonic acid from neutrophil membranes. It inhibits mitogen-induced stimulation of peripheral blood mononuclear cells. This chemical stabilizes lysosomal membranes in macrophages and inhibits Mycobacterium leprae metabolism in mouse peritoneal macrophages. It (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. This compound inhibits 90% of twenty M. tuberculosis strains with MICs <1.0 μg/mL, to be noted, it inhibits M. tuberculosis strain 2227 with MICs of 0.06 μg/mL. It (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. This compound (500 μg, bid) results in highest Clofazimine concentrations in spleens and livers of mice whereas Clofazimine concentrations in the lungs are significantly lower. This chemical (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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10390215/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10629016/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-20)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07485010 NOT_YET_RECRUITING
Mycobacterium Abscessus Pulmonary Disease; Mycobacterium Abscessus Infection; Non-Tuberculous Mycobacterial (NTM) Infections; Non-Tuberculous Mycobacteria Pulmonary Disease
The University of Queensland
2027-04 PHASE2
NCT04310930 RECRUITING
Pulmonary Disease Due to Mycobacteria (Diagnosis)
The University of Queensland
2020-03-02 PHASE2; PHASE3
NCT07228702 ENROLLING_BY_INVITATION
Non-Tuberculous Mycobacterial (NTM) Pneumonia; Mycobacterium Abscessus Infection
Vancouver Coastal Health
2026-01-11 PHASE1
NCT07198685 NOT_YET_RECRUITING
Treat to Target; Treatment Duration
Wuhan Pulmonary Hospital
2025-09-30
NCT07126639 NOT_YET_RECRUITING
Efficacy and Safety
Wuhan Pulmonary Hospital
2025-09-01
NCT03828201 ACTIVE_NOT_RECRUITING
Tuberculosis, Multidrug-Resistant
Boston University
2022-06-07 PHASE2

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