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Clofazimine

Catalog No. T0377   CAS 2030-63-9
Synonyms: NSC-141046

Clofazimine (NSC-141046) is a phenazine dye with anti-mycobacterial and anti-inflammatory activities. Clofazimine has a slow bactericidal effect on Mycobacterium leprae and is active against various other Mycobacteria.

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Clofazimine Chemical Structure
Clofazimine, CAS 2030-63-9
Pack Size Availability Price/USD Quantity
500 mg In stock $ 50.00
1 mL * 10 mM (in DMSO) In stock $ 55.00
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Purity: 99.79%
Purity: 99.2%
Purity: 99.18%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Clofazimine (NSC-141046) is a phenazine dye with anti-mycobacterial and anti-inflammatory activities. Clofazimine has a slow bactericidal effect on Mycobacterium leprae and is active against various other Mycobacteria.
In vitro Administered bi-daily at 500 μg, Clofazimine accumulates at the highest concentrations in the spleen and liver, while significantly reduced levels are observed in the lungs. A dosage of 20 mg/kg of Clofazimine can prevent death by significantly decreasing the colony-forming unit (CFU) count in the lungs and spleen of C57BL/6 mice infected with the tuberculosis bacillus Mycobacterium tuberculosis H37Rv. The same dosage effectively lowers bacterial numbers in the liver, spleen, and lungs of C57BL/6 mice infected with the Mycobacterium avium strain TMC724. Moreover, 50 mg/kg of Liposomal Clofazimine in acute infection reduces CFUs in the spleen, liver, and lungs of mice harboring the Erdman strain of tuberculosis, exhibiting dose-dependency.
In vivo At a concentration of 1 μg/mL, Clofazimine inhibits the activity of J774A.1 macrophages in a dose-dependent manner. The compound targets neutrophils, activating phospholipase A2 which, in turn, increases the release of lysophosphatidylcholine and arachidonic acid from the neutrophil membrane. In macrophages, Clofazimine stabilizes lysosomal membranes and impedes the metabolism of Mycobacterium leprae within murine peritoneal macrophages. Additionally, Clofazimine exhibits a 90% inhibition rate on 20 strains of Mycobacterium tuberculosis with minimum inhibitory concentrations (MICs) of less than 1.0 μg/mL. It also suppresses the mitogen-induced proliferation of peripheral blood mononuclear cells.
Synonyms NSC-141046
Molecular Weight 473.4
Formula C27H22Cl2N4
CAS No. 2030-63-9

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 1mg/ml, Sonication is recommended.

TargetMolReferences and Literature

1. Arbiser JL, et al. J Am Acad Dermatol, 1995, 32(2 Pt 1), 241-247. 2. Van Rensburg CE, et al. Antimicrob Agents Chemother, 1992, 36(12), 2729-2735. 3. Reddy VM, et al. Antimicrob Agents Chemother, 1996, 40(3), 633-636. 4. Adams LB, et al. Antimicrob Agents Chemother, 1999, 43(7), 1638-1643. 5. Peters K, et al. J Antimicrob Chemother, 2000, 45(1), 77-83. 6. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth[J]. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144.

TargetMolCitations

1. Bowden G D, Land K M, O'Connor R M, et al. High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth. International Journal for Parasitology: Drugs and Drug Resistance. 2018 Apr;8(1): 137-144

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library FDA-Approved Drug Library Bioactive Compounds Library Max Pediatric Drug Library Approved Drug Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

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Keywords

Clofazimine 2030-63-9 DNA Damage/DNA Repair Microbiology/Virology Antibiotic Antibacterial DNA NSC-141046 NSC 141046 Inhibitor NSC141046 Bacterial inhibit inhibitor

 

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