Clofazimine

SKU: orb1310671

Description

Clofazimine is a phenazine-derived small molecule with bactericidal activity against Mycobacterium leprae and broad-spectrum anti-mycobacterial properties. It is utilized in research for studying tuberculosis and leprosy, both in vitro and in animal models, due to its combined antimicrobial and anti-inflammatory effects.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 2030-63-9
• MW: 473.4
• Purity: 99.85% (May vary between batches)
• Formula: C₂₇H₂₂Cl₂N₄
• SMILES: N(C(C)C)=C1C=C2N(C=3C(N=C2C=C1NC4=CC=C(Cl)C=C4)=CC=CC3)C5=CC=C(Cl)C=C5
• Target: DNA/RNA Synthesis,Antibacterial,DNA,Antibiotic,Apoptosis,Interleukin
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:2.64 mg/mL (5.58 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Clofazimine, DNA, Bacterial, Antibiotic, inhibit, NSC 141046, NSC141046, NSC-141046, Inhibitor

Compound Identifiers

PubChem CID

2794