2. Anti-infection Cell Cycle/DNA Damage Immunology/Inflammation Apoptosis
  3. Bacterial Antibiotic DNA/RNA Synthesis Interleukin Related Apoptosis
  4. Clofazimine

Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research.

For research use only. We do not sell to patients.

Clofazimine Chemical Structure

Clofazimine Chemical Structure

CAS No. : 2030-63-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 66 In-stock
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10 mM * 1 mL in DMSO USD 66 In-stock
Solid
500 mg USD 60 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Clofazimine:

Clofazimine Related Antibodies

Top Publications Citing Use of Products

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research[1][2][3][4][5].

IC50 & Target

Quinolone

 

In Vitro

Clofazimine (0.0625-2 mg/L, 14 d) exerts no apparent activity against M. tuberculosis during the first 2–4 days of exposure, exhibits a concentration-dependent antimicrobial activity after 1 week: bacteriostatic activity at concentrations at or below the 0.25 mg/L MIC and bactericidal activity at concentrations above the MIC. INH is used as positive control.[3].
Clofazimine (10 μM, 24 h) inhibits the growth of hematological cancer cell lines (Jurkat, U266, Namalwa, K562, HL60). For U266, Clofazimine (1-50 μM, 12-48 h) shows a dose- and time-dependent inhibitory effect[4].
Clofazimine (10 μM, 24-48 h) depolarizes the mitochondrial membrane, significantly increases active caspase-3 level (25-fold) and increases the percentage of early and late apoptotic cells in U266[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clofazimine Related Antibodies
In Vivo

Clofazimine (100,50 mg/kg, p.o., once per day for 14 d) exhibits a delayed antimicrobial activity against Mycobacterium tuberculosis in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (age 6–8 weeks, mass 18–20 g)[3]
Dosage: 100, 50, 25, 12.5, 6.25, 3.125 or 1.5625 mg/kg
Administration: Oral gavage (p.o.), once per day for 14 d
Result: Exhibited an increase of the lung bacterial load during the first 7 days of treatment, and decreased the CFU counts in the lungs of mice after 10 days of treatment.
Significantly declined the lung CFU counts in 100 or 50 mg/ kg group at 14th day.
Clinical Trial
Molecular Weight

473.40

Formula

C27H22Cl2N4
CAS No.
Appearance

Solid

Color

Pink to red

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (13.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.62 mg/mL (1.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 0.62 mg/mL (1.31 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.62 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 1.67 mg/mL (3.53 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 1.67 mg/mL (3.53 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

COA (251 KB) RP-HPLC (244 KB) MS (68 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1124 mL 10.5619 mL 21.1238 mL 52.8095 mL
5 mM 0.4225 mL 2.1124 mL 4.2248 mL 10.5619 mL
10 mM 0.2112 mL 1.0562 mL 2.1124 mL 5.2809 mL
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Clofazimine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Clofazimine2030-63-9BacterialAntibioticDNA/RNA SynthesisInterleukin RelatedApoptosisILMycobacterialleprosytuberculosisanti-inflammatoryDNA replicationJurkatBALB/c miceM. tuberculosis strain H37RvHL60NamalwaK562U266Inhibitorinhibitorinhibit

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