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Isoniazid Fatty Acid Synthase inhibitor

Cat.No.S1937

Isoniazid is a prodrug that blocks the action of fatty acid synthase by interacting with KatG, used for the prevention and treatment of tuberculosis.
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Quality Control

Batch: Purity: 99.83%
99.83

Solubility

In vitro
Batch:

DMSO : 27 mg/mL (196.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 27 mg/mL

Ethanol : 27 mg/mL

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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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Chemical Information, Storage & Stability

Molecular Weight 137.14 Formula

C6H7N3O

Storage (From the date of receipt)
CAS No. 54-85-3 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES C1=CN=CC=C1C(=O)NN

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

In vitro
Isoniazid is a prodrug that requires activation by the mycobacterial catalase-peroxidase enzyme (KatG) to an active form that then exerts a lethal effect on an intracellular target or targets. This compound upregulates the expression of an operon containing five FAS II components, including kasA and acpM. It results in the accumulation of ACP-bound lipid precursors to mycolic acids that are 26 carbons long and fully saturated. This chemical enters the mycobacterial cell by passive diffusion. It itself is not toxic to the bacterial cell, but acts as a prodrug and is activated by the mycobacterial enzyme KatG, a multifunctional catalase-peroxidase that has other activities, including peroxynitritase and NADH oxidase. The agent inhibits cell wall lipid synthesis, coupled with the findings that inhibitory INH adducts of NAD+/NADP+ are formed from the isonicotinoyl radical, leading the field away from this area. It induces a concentration-dependent (0-40 mM) cytotoxic effect in day-1 treated HepG2 cells and not significantly affected by decreases in intracellular GSH concentrations.
In vivo
Isoniazid increases CYP2E1 protein, and the 6-hydroxychlorzoxazone formation rate is increased by 2.7 and 2.2-fold in liver and kidney, respectively. This compound decreases liver and kidney 20-HETE content to 34% and 15.6% of control, respectively, without significantly altering tissue 19-HETE concentration.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9023573/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15205388/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-03-17)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03785106 ACTIVE_NOT_RECRUITING
HIV-infected Participants With Latent TB Infection in High TB Burden Country
The HIV Netherlands Australia Thailand Research Collaboration
2019-08-15 PHASE3
NCT07656012 NOT_YET_RECRUITING
Tuberculosis
University of Wisconsin, Madison
2026-09 PHASE2
NCT07076225 NOT_YET_RECRUITING
Pulmonary Tuberculosis
Shenzhen Third People's Hospital
2025-07-25 PHASE3
NCT03474029 RECRUITING
Latent Tuberculosis
Centers for Disease Control and Prevention
2019-08-01 PHASE2; PHASE3
NCT07595042 NOT_YET_RECRUITING
Tuberculosis
National Institute of Allergy and Infectious Diseases (NIAID)
2026-10-30 PHASE2
NCT06526221 ENROLLING_BY_INVITATION
Tuberculosis, Pulmonary; Medication Adherence
Tufts University
2026-04-07

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