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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.
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| References |
J Am Acad Dermatol.1995 Feb;32(2 Pt 1):241-7;Antimicrob Agents Chemother.1996 Mar;40(3):633-36.
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| Additional Infomation |
Clofazimine is 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients. It has a role as a leprostatic drug, a non-steroidal anti-inflammatory drug and a dye. It is a member of phenazines and a member of monochlorobenzenes.
Clofazimine is an Antimycobacterial. Clofazimine has been reported in Streptomyces hygroscopicus with data available. 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. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619) See also: Clofazimine (annotation moved to). |
| Molecular Formula |
C27H22CL2N4
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| Molecular Weight |
473.4
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| Exact Mass |
472.122
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| CAS # |
2030-63-9
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| Related CAS # |
Clofazimine-d7
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| PubChem CID |
2794
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| Appearance |
Pink to red solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
566.9±50.0 °C at 760 mmHg
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| Melting Point |
210-212°
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| Flash Point |
296.7±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.667
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| LogP |
7.26
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
829
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WDQPAMHFFCXSNU-BGABXYSRSA-N
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| 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+
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| Chemical Name |
N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| 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.
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.
| 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 |
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