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

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
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
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 0.62 mg/mL (1.31 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
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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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

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.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05294146 Completed Drug: Clofazimine Nontuberculous Mycobacterial
Diseases
Radboud University Medical Center February 14, 2022 Phase 2
NCT03341767 Terminated Drug: Clofazimine
Drug: Placebo
Cryptosporidiosis University of Washington December 14, 2017 Phase 2
NCT02968212 Recruiting Drug: Clofazimine
Other: sugar pill
Mycobacterium Avium Complex Oregon Health and Science University April 11, 2017 Phase 2
NCT01290744 Completed Drug: Clofazimine
Drug: Placebo
Borderline Lepromatous Leprosy
Lepromatous Leprosy
Paul Saunderson August 2010 Phase 4
Biological Data
  • In vitro activity of isoniazid (a–c) and clofazimine (d–f) against M. tuberculosis. Data are shown from three biological replicates (a and d, b and e, and c and f represent the replicate groups). The broken line represents the log10 cfu/mL at the start of the experiment. The number following the drug abbreviation (INH, isoniazid; CLO, clofazimine) represents the drug concentration in mg/L.
  • In vivo EBA of isoniazid and clofazimine. (a) Serum clofazimine concentration in mice after 14 days of administration. The broken line represents the MIC of clofazimine for M. tuberculosis (0.25 mg/L). (b) cfu counts in the lungs of mice after infection (day −6), at the start of treatment (day 0) and during treatment. The number following the drug abbreviation (INH, isoniazid; CLO, clofazimine) represents the daily drug dose in mg/kg. For both graphs, data represent the mean (five mice per group) and error bars represent the SD.
  • Clofazimine inhibits IL-2 production and NFAT activation in Jurkat T cells.
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