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  4. Ethambutol

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.

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

Ethambutol Chemical Structure

Ethambutol Chemical Structure

CAS No. : 74-55-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Ethambutol:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ethambutol

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases. Target: Antibacterial Ethambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].

Cellular Effect
Cell Line Type Value Description References
BMDM CC50
100 μg/mL
Compound: Ethambutol
Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability after 24 hrs by MTS assay
Cytotoxicity against Swiss mouse BMDM assessed as reduction in cell viability after 24 hrs by MTS assay
[PMID: 28712709]
HepG2 CC50
> 400 μg/mL
Compound: EMB
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33940463]
MRC5 CC50
> 10 μg/mL
Compound: EMB
Cytotoxicity against human MRC5 cells after 24 hrs
Cytotoxicity against human MRC5 cells after 24 hrs
[PMID: 26254828]
RAW264.7 CC50
≥ 400 μg/mL
Compound: EMB
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33940463]
THP-1 EC50
5.38 mg/L
Compound: Ethambutol
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing after 7 days
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as extracellular bacterial killing after 7 days
[PMID: 20231389]
THP-1 EC50
7.93 mg/L
Compound: Ethambutol
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing after 7 days
Antimycobacterial activity against Mycobacterium avium ATCC 700898 infected in human THP1 cells assessed as intracellular bacterial killing after 7 days
[PMID: 20231389]
Vero IC50
> 150 μg/mL
Compound: ethambutol
Cytotoxicity against Vero cells after 48 hrs by XTT method
Cytotoxicity against Vero cells after 48 hrs by XTT method
[PMID: 17888665]
Vero CC50
> 188.5 μM
Compound: Ethambutol
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells assessed as cell viability after 72 hr by MTT assay
Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells assessed as cell viability after 72 hr by MTT assay
10.1007/s00044-011-9638-9
Vero IC50
> 200 μg/mL
Compound: EMB
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 30145051]
Vero IC50
> 305.9 μM
Compound: Ethambutol
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 19942326]
Vero IC50
> 305.9 μM
Compound: ethambutol
Cytotoxicity against Vero cells after 72 hrs by MTT assay
Cytotoxicity against Vero cells after 72 hrs by MTT assay
[PMID: 17276683]
Vero IC50
> 50 μg/mL
Compound: Ethambutol
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 24044875]
Vero CC50
> 500 μM
Compound: EMB
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
[PMID: 22626551]
Vero IC50
> 6.25 μg/mL
Compound: Ethambutol
Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay
[PMID: 28552337]
Vero IC50
> 62.5 μg/mL
Compound: Ethambutol
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 24721315]
Vero IC50
> 62.5 μg/mL
Compound: Ethambutol
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 23352268]
Vero CC50
1470 μM
Compound: EMB
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 21376586]
Vero CC50
38.51 μg/mL
Compound: A, ETB
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by resazurin assay
[PMID: 23474387]
Vero IC50
390.93 μg/mL
Compound: EMB
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue staining based assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue staining based assay
[PMID: 28844400]
In Vivo

Induction of Hyperuricaemic Disease[4][5]

Background
Elevated uric acid levels can lead to crystal deposition and may cause gout, urolithiasis, and urate nephropathy. Ethambutol can cause increased uric acid levels by reducing renal uric acid clearance, ultimately leading to hyperuricemia[4][5].
Specific Mmodeling Methods
Rat[4]: male • Wistar rats • SPF • 200-220 g
Administrtion: 250 mg/kg • intragastric administration • once daily for 23 days
Note
Modeling Record
Pathological changes: Pathological damage and inflammatory reaction in the thymus and spleen; thymus atrophy, cortical medullary fusion; splenic sinus congestion, with iron yellow deposition.
Physiological changes: serum uric acid level ↑; sparse cells, increased number of tissue cells, and decreased number of lymphocytes.
Molecular changes: URAT1 level ↑, OAT1 level ↓ in kidney homogenate.
Correlated Product(s): Xanthine Oxidase Inhibitors

Induction of Optic Neuropathy[6]

Background
Ethambutol treatment can cause binocular toxicity at certain doses and durations. There is currently no clear treatment to prevent damage to retinal neuronal cells in cases of ethhambutol-induced optic neuropathy (EON).
Specific Mmodeling Methods
Rat[6]: Wistar rats • Administration: 35 mg/kg/day &bull po for 30 days
Note
Modeling Record
Molecular changes: Bcl-2, Caspase-3 expression levels ↑.
Pathological indicators: Ganglion cell damage, increased density of retinal ganglion cells (RGC); RGC cell layer thickened due to vacuoles formed in the ganglion cell cytoplasm.
Correlated Product(s): Citicoline (HY-B0739)

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

Clinical Trial
Molecular Weight

204.31

Formula

C10H24N2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@H](NCCN[C@@H](CC)CO)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (489.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8945 mL 24.4726 mL 48.9452 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8945 mL 24.4726 mL 48.9452 mL 122.3631 mL
5 mM 0.9789 mL 4.8945 mL 9.7890 mL 24.4726 mL
10 mM 0.4895 mL 2.4473 mL 4.8945 mL 12.2363 mL
15 mM 0.3263 mL 1.6315 mL 3.2630 mL 8.1575 mL
20 mM 0.2447 mL 1.2236 mL 2.4473 mL 6.1182 mL
25 mM 0.1958 mL 0.9789 mL 1.9578 mL 4.8945 mL
30 mM 0.1632 mL 0.8158 mL 1.6315 mL 4.0788 mL
40 mM 0.1224 mL 0.6118 mL 1.2236 mL 3.0591 mL
50 mM 0.0979 mL 0.4895 mL 0.9789 mL 2.4473 mL
60 mM 0.0816 mL 0.4079 mL 0.8158 mL 2.0394 mL
80 mM 0.0612 mL 0.3059 mL 0.6118 mL 1.5295 mL
100 mM 0.0489 mL 0.2447 mL 0.4895 mL 1.2236 mL
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    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.

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Product Name:
Ethambutol
Cat. No.:
HY-B0535
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