product name Clofazimine
Description: Clofazimine is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity. Clofazimine is a fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients.
References: J Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7; Antimicrob Agents Chemother. 1996 Mar;40(3):633-36.
473.4
Formula
C27H22Cl2N4
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
Solubility (In vivo)
Synonyms
NSC-141046
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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 model | |
| Formulation & Dosage | |
| References | J Am Acad Dermatol. 1995 Feb;32(2 Pt 1):241-7; Antimicrob Agents Chemother. 1996 Mar;40(3):633-36. |
