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MedKoo Cat#: 317551 | Name: Clofazimine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. Clofazimine works by binding to the guanine bases of bacterial DNA, thereby blocking the template function of the DNA and inhibiting bacterial proliferation.

Chemical Structure

Clofazimine
Clofazimine
CAS#2030-63-9 (free base)

Theoretical Analysis

MedKoo Cat#: 317551

Name: Clofazimine

CAS#: 2030-63-9 (free base)

Chemical Formula: C27H22Cl2N4

Exact Mass: 472.1222

Molecular Weight: 473.40

Elemental Analysis: C, 68.50; H, 4.68; Cl, 14.98; N, 11.84

Price and Availability

Size Price Availability Quantity
1g USD 110.00 Ready to ship
2g USD 150.00 Ready to ship
5g USD 300.00 Ready to ship
10g USD 450.00 Ready to ship
25g USD 750.00 Ready to ship
50g USD 1,250.00 Ready to ship
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Related CAS #
352464-74-5 (nitrate) 2030-63-9 (free base)
Synonym
Clofazimine; Chlofazimine; B 663; B 663; B-663; G 30320; Lampren; Lamprene; NSC 141046; NSC-141046;
IUPAC/Chemical Name
N,5-bis(4-chlorophenyl)-3-propan-2-yliminophenazin-2-amine
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+
SMILES Code
CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl
Appearance
Reddish-brown solid powder.
Purity
>95% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO (8mg/mL)
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Solvent mg/mL mM comments
Solubility
DMSO 4.0 8.45
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 473.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Fukutomi Y, Maeda Y, Makino M. Apoptosis-inducing activity of clofazimine in macrophages. Antimicrob Agents Chemother. 2011 Sep;55(9):4000-5. doi: 10.1128/AAC.00434-11. Epub 2011 Jun 20. PMID: 21690278; PMCID: PMC3165281. 2. Ahmad S, Bhattacharya D, Gupta N, Rawat V, Tousif S, Van Kaer L, Das G. Clofazimine enhances the efficacy of BCG revaccination via stem cell-like memory T cells. PLoS Pathog. 2020 May 21;16(5):e1008356. doi: 10.1371/journal.ppat.1008356. PMID: 32437421; PMCID: PMC7269335. 3. . Tuvshintulga B, AbouLaila M, Davaasuren B, Ishiyama A, Sivakumar T, Yokoyama N, Iwatsuki M, Otoguro K, Ōmura S, Igarashi I. Clofazimine Inhibits the Growth of Babesia and Theileria Parasites In Vitro and In Vivo. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2739-46. doi: 10.1128/AAC.01614-15. PMID: 26883713; PMCID: PMC4862543. 4. Swanson RV, Ammerman NC, Ngcobo B, Adamson J, Moodley C, Dorasamy A, Moodley S, Mgaga Z, Bester LA, Singh SD, Almeida DV, Grosset JH. Clofazimine Contributes Sustained Antimicrobial Activity after Treatment Cessation in a Mouse Model of Tuberculosis Chemotherapy. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2864-9. doi: 10.1128/AAC.00177-16. PMID: 26926638; PMCID: PMC4862514
In vitro protocol:
1. Fukutomi Y, Maeda Y, Makino M. Apoptosis-inducing activity of clofazimine in macrophages. Antimicrob Agents Chemother. 2011 Sep;55(9):4000-5. doi: 10.1128/AAC.00434-11. Epub 2011 Jun 20. PMID: 21690278; PMCID: PMC3165281. 2. Ahmad S, Bhattacharya D, Gupta N, Rawat V, Tousif S, Van Kaer L, Das G. Clofazimine enhances the efficacy of BCG revaccination via stem cell-like memory T cells. PLoS Pathog. 2020 May 21;16(5):e1008356. doi: 10.1371/journal.ppat.1008356. PMID: 32437421; PMCID: PMC7269335.
In vivo protocol:
1. Tuvshintulga B, AbouLaila M, Davaasuren B, Ishiyama A, Sivakumar T, Yokoyama N, Iwatsuki M, Otoguro K, Ōmura S, Igarashi I. Clofazimine Inhibits the Growth of Babesia and Theileria Parasites In Vitro and In Vivo. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2739-46. doi: 10.1128/AAC.01614-15. PMID: 26883713; PMCID: PMC4862543. 2. Swanson RV, Ammerman NC, Ngcobo B, Adamson J, Moodley C, Dorasamy A, Moodley S, Mgaga Z, Bester LA, Singh SD, Almeida DV, Grosset JH. Clofazimine Contributes Sustained Antimicrobial Activity after Treatment Cessation in a Mouse Model of Tuberculosis Chemotherapy. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2864-9. doi: 10.1128/AAC.00177-16. PMID: 26926638; PMCID: PMC4862514.
1: Ferro BE, Meletiadis J, Wattenberg M, de Jong A, van Soolingen D, Mouton JW, van Ingen J. Clofazimine prevents the regrowth of Mycobacterium abscessus and Mycobacterium avium type strains exposed to amikacin and clarithromycin. Antimicrob Agents Chemother. 2015 Dec 7. pii: AAC.02615-15. [Epub ahead of print] PubMed PMID: 26643335. 2: Jarand J, Davis JP, Cowie RL, Field SK, Fisher DA. Long Term Follow Up Of Mycobacterium Avium Complex Lung Disease In Patients Treated With Regimens Including Clofazimine and/or Rifampin. Chest. 2015 Oct 29. doi: 10.1378/chest.15-0543. [Epub ahead of print] PubMed PMID: 26513209. 3: López-Gavín A, Tudó G, Vergara A, Hurtado JC, Gonzalez-Martín J. In vitro activity against Mycobacterium tuberculosis of levofloxacin, moxifloxacin and UB-8902 in combination with clofazimine and pretomanid. Int J Antimicrob Agents. 2015 Nov;46(5):582-5. doi: 10.1016/j.ijantimicag.2015.08.004. Epub 2015 Sep 7. PubMed PMID: 26421981. 4: Officioso A, Alzoubi K, Manna C, Lang F. Clofazimine Induced Suicidal Death of Human Erythrocytes. Cell Physiol Biochem. 2015;37(1):331-41. doi: 10.1159/000430357. Epub 2015 Aug 24. PubMed PMID: 26316080. 5: Faouzi M, Starkus J, Penner R. State-dependent blocking mechanism of Kv 1.3 channels by the antimycobacterial drug clofazimine. Br J Pharmacol. 2015 Nov;172(21):5161-73. doi: 10.1111/bph.13283. Epub 2015 Oct 9. PubMed PMID: 26276903. 6: Baijnath S, Naiker S, Shobo A, Moodley C, Adamson J, Ngcobo B, Bester LA, Singh S, Kruger HG, Naicker T, Govender T. Evidence for the presence of clofazimine and its distribution in the healthy mouse brain. J Mol Histol. 2015 Oct;46(4-5):439-42. doi: 10.1007/s10735-015-9634-3. Epub 2015 Jul 25. PubMed PMID: 26208572. 7: Roy K, Sil A, Das NK, Bandyopadhyay D. Effectiveness and safety of clofazimine and pentoxifylline in type 2 lepra reaction: a double-blind, randomized, controlled study. Int J Dermatol. 2015 Nov;54(11):1325-32. doi: 10.1111/ijd.12793. Epub 2015 Jun 20. PubMed PMID: 26094723. 8: Zhang S, Chen J, Cui P, Shi W, Zhang W, Zhang Y. Identification of novel mutations associated with clofazimine resistance in Mycobacterium tuberculosis. J Antimicrob Chemother. 2015 Sep;70(9):2507-10. doi: 10.1093/jac/dkv150. Epub 2015 Jun 4. PubMed PMID: 26045528; PubMed Central PMCID: PMC4539095. 9: Converse PJ, Tyagi S, Xing Y, Li SY, Kishi Y, Adamson J, Nuermberger EL, Grosset JH. Efficacy of Rifampin Plus Clofazimine in a Murine Model of Mycobacterium ulcerans Disease. PLoS Negl Trop Dis. 2015 Jun 4;9(6):e0003823. doi: 10.1371/journal.pntd.0003823. eCollection 2015 Jun. PubMed PMID: 26042792. 10: Lechartier B, Cole ST. Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Aug;59(8):4457-63. doi: 10.1128/AAC.00395-15. Epub 2015 May 18. PubMed PMID: 25987624; PubMed Central PMCID: PMC4505229.

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