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    InvivoChem Cat #: V0840
    CAS #: 2030-63-9Purity ≥98%

    Description: Clofazimine (B-663; G-30320; NSC-141046; Lamprene; Lampren; Chlofazimine; Clofazimina), an antibacterial drug, is a rhimophenazine-based dye that is fat-soluble, and was originally developed as an anti-TB/tuberculosis drug but now used for treating leprosy. Clofazimine has antimicrobial and antiinflammatory activity, and has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine was approved for clinical use in the US in 1986.  

    References: J Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7; Antimicrob Agents Chemother. 1996 Mar;40(3):633-36.

    Related CAS #: 2030-63-9 (free base); 352464-74-5 (nitrate) 

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    • 香港大学
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    Molecular Weight (MW)473.4
    CAS No.2030-63-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (10.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine
    InChi Code: InChI=1S/C27H22Cl2N4/c1-17(2)30-24-16-27-25(15-23(24)31-20-11-7-18(28)8-12-20)32-22-5-3-4-6-26(22)33(27)21-13-9-19(29)10-14-21/h3-17,31H,1-2H3/b30-24+
    SMILES Code: CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl
    SynonymsB 663; B 663; G 30320; G-30320; NSC-141046; NSC141046; B-663; G30320; NSC 141046; Clofazimine; Lamprene; Lampren; Chlofazimine; Clofazimina

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    In Vitro

    In vitro activity: 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. 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. 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.

    Cell Assay: Clofazimine is a fat-soluble iminophenazine dye, has a marked anti-inflammatory effect, has been used in combination with other antimycobacterial drugs to treat AIDS and Crohn's disease.

    In VivoClofazimine (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. 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.
    Animal modelMice
    Formulation & Dosage20 mg/kg
    ReferencesJ Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7; Antimicrob Agents Chemother. 1996 Mar;40(3):633-36.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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