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Ethionamide

Synonyms: Bayer 5312

Ethionamide (Bayer 5312) is an antibiotic used in the treatment of tuberculosis.

Ethionamide Chemical Structure

Ethionamide Chemical Structure

CAS No. 536-33-4

Purity & Quality Control

Ethionamide Related Products

Biological Activity

Description Ethionamide (Bayer 5312) is an antibiotic used in the treatment of tuberculosis.
In vitro
In vitro Ethionamide is a structural analogue of isoniazid (INH), both are pro-drugs that need to be activated by mycobacterial enzymes to exert their antimicrobial activity. Ethionamide mechanism of action is thought to be identical to INH although the pathway of activation is distinct from that of INH. Ethionamide is activated by an EthA enzyme, leading to the formation of a Soxide metabolite that has considerably better activity than the parent drug. [1] Ethionamide inhibits both biofilm formation and viability of mature biofilms. Ethionamide reduces the content of ergosterol in Cryptococcus spp. planktonic cells and destabilized or permeabilized the fungal cell membrane, leading to leakage of macromolecules. [2] Ethionamide is in general toxic at concentrations above 0.50 mM to HepG2, Caco-2, and RAW macrophage cells, but the toxicity is drastically reduced when Ethionamide is loaded into the microparticles. Ethionamide shows a fast metabolization process in the presence of the thermally carbonized- Porous silicon (TCPSi) particles. [3] Ethionamide is activated in Mycobacterium tuberculosis by the protein encoded by the gene Rv3854c. Ethionamide appear to disrupt cell wall biosynthesis and have at least one common cellular target, the enoyl-acyl carrier protein reductase InhA. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05258877 Completed
Tuberculosis Pulmonary
BioVersys AG|TASK Applied Science
 June 10 2022 --

Chemical Information & Solubility

Molecular Weight 166.24 Formula

C8H10N2S
CAS No. 536-33-4 SDF Download Ethionamide SDF
Smiles CCC1=NC=CC(=C1)C(=S)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 33 mg/mL ( (198.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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