| CAS |
2030-63-9 |
| Chinese Name |
氯苯吩嗪 |
| English Name |
Clofazimine |
| Synonyms |
氯法齐明;氯苯吩嗪; |
| Molecular Formula |
C27H22Cl2N4 |
| Molecular Weight |
473.4 |
| Solubility |
Soluble in DMSO ≥1mg/mL(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 217-980-2 |
| MDL |
MFCD00056793 |
| 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 |
| InChIKey |
WDQPAMHFFCXSNU-UHFFFAOYSA-N |
| InChI |
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 |
| PubChem CID |
2794 |
| Target Point |
Others |
| Passage |
Immunology & Inflammation |
| Background |
Clofazimine is a rhimophenazine dye with antibacterial and anti-inflammatory activity. |
| Biological Activity |
Clofazimine(CFM; also known as B663 or Lamprene) was developed initially as an antituberculosis drug (1–3). In the earlier experimental tuberculosis studies with hamster and mouse models, the drug was found to be effective. Subsequently, on the basis of the fact that it concentrates extensively inside macrophages and on the basis of the logic of using an intracellular drug on an intracellular parasite, CFM has been used successfully for the treatment of leprosy. [1] |
| In Vitro |
The MICs of B4154，B4157，and CFM at which 90% of strains were inhibited were 0.25，0.12，and < or = 1.0 microgram/ml，respectively. The intracellular activities of CFM and B4157 were superior to that of B4154. [1] |
| In Vivo |
At a dose of 20 mg/kg of body weight，the activity of CFM was slightly superior to that of B4157; CFM prevented mortality and caused a significant reduction in the numbers of CFU in the lungs and spleens. The chemotherapeutic activity of CFM was comparable to those of rifampin and isoniazid. Complete susceptibility of multidrug-resistant strains to CFM and B4157 and the therapeutic efficacies of these compounds against mouse tuberculosis make these drugs attractive agents for the treatment of drug-resistant tuberculosis.[1] |
| Cell Experiment |
Macrophages were scraped from culture plates and washed once，and viability was determined by trypan blue exclusion. Twenty-four-well tissue culture plates were seeded with 106 cells per well，and the plates were incubated for 2 h at 378 C in a CO2 incubator. Nonadherent cells were washed off with warm Hanks’ saline. The adherent monolayer of macrophages was infected with an M. tuberculosis H37Rv suspension in DMEM(about 107 CFU/ml)prepared as described above. After 2h of incubation，the wells were washed three times with warm Hanks’ saline and the contents of the wells were replaced with DMEM containing 1% fetal calf serum and different concentrations of the drugs(1.0，0.5，and 0.25 m g of CFM and its analogs per ml and 0.1 m g of isoniazid per ml). Control wells received drug-free medium. The macrophage cultures were incubated at 378 C in a CO2 incubator for 4 days. At days 0 and 4，the contents of triplicate wells in each group were lysed with 0.25% sodium dodecyl sulfate. Aliquots of the lysates were inoculated into BACTEC vials，and the results were read after 24 h.[1] |
| Animal Experiment |
C57BL/6 mice were infected intravenously through a lateral caudal vein with mouse-passaged M. tuberculosis H37Rv in 0.2 ml containing approximately 106 CFU. On the next day，three mice were killed and the rest of the mice were divided into groups and dosed with different drugs for 8 to 12 weeks. CFM and its analogs were given at a dose of 20 mg/kg of body weight，isoniazid was given at a dose of 25 mg/kg，and rifampin was given at a dose of 25 mg/kg. Unless otherwise mentioned，the drugs were given 5 days a week and were not given on the day before the mice were killed. At 4，8，and 12 weeks after treatment，three mice in each group were killed. Their lungs and spleens were collected aseptically and were homogenized in 10 ml of saline.[1] |
| Data Literature Source |
[1]. Reddy VM，Nadadhur G，Daneluzzi D，O'Sullivan JF，Gangadharam PR. Antituberculosis activities of clofazimine and its new analogs B4154 and B4157. Antimicrob Agents Chemother. 1996 Mar;40(3):633-36. |
| Unit |
Bottle |
| Specification |
250mg 500mg 1g |
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