Clofazimine

Alias: B 663; B 663; G 30320;G-30320;NSC-141046;NSC141046;B-663;G30320; NSC 141046;Clofazimine; Lamprene; Lampren; Chlofazimine; Clofazimina
Cat No.:V0840 Purity: ≥98%
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 Chemical Structure CAS No.: 2030-63-9
Product category: Phospholipase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
25g
Other Sizes
Official Supplier of:
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Product 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.

Biological Activity I Assay Protocols (From Reference)
ln 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 Crohns disease.

ln 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 Protocol
20 mg/kg
Mice
References
J 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.
Physicochemical Properties
Molecular Formula
C27H22CL2N4
Molecular Weight
473.4
CAS #
2030-63-9
Related CAS #
Clofazimine-d7
SMILES
CC(/N=C1C(NC2=CC=C(Cl)C=C2)=CC3=NC4=C(C=CC=C4)N(C5=CC=C(Cl)C=C5)C3=C/1)C
InChi Key
WDQPAMHFFCXSNU-BGABXYSRSA-N
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+
Chemical Name
N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine
Synonyms
B 663; B 663; G 30320;G-30320;NSC-141046;NSC141046;B-663;G30320; NSC 141046;Clofazimine; Lamprene; Lampren; Chlofazimine; Clofazimina
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 5 mg/mL (10.6 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1124 mL 10.5619 mL 21.1238 mL
5 mM 0.4225 mL 2.1124 mL 4.2248 mL
10 mM 0.2112 mL 1.0562 mL 2.1124 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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