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5.34342 Sigma-Aldrich

InhA Inhibitor, NITD-916 - Calbiochem

Synonym: 6-((4,4-dimethylcyclohexyl)methyl)-4-hydroxy-3-phenylpyridin-2(1H)-one , Enoyl-acyl Carrier Protein Reductase Inhibitor, NITD-916, Enoyl-ACP reductase, NITD-916, InhA Inhibitor, NITD-916 - Calbiochem

  • Empirical Formula (Hill Notation) C20H25NO2

  • Molecular Weight 311.42

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Properties

Related Categories Antibiotics, Antiviral, Biochemicals and Reagents, Spectrum of Activity
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   white
solubility   DMSO: 10 mg/mL

Description

General description

A cell-permeable, orally available, highly lipophilic 4-hydroxy-2-pyridone derivative that directly binds to the enoyl-substrate binding pocket of Mycobaterial enoyl reductase inhA in an NADH-dependent manner and inhibits its activity (IC50 = 570 nM). Shown to be about 5 to 8 times more potent ((MIC50 = 40 to 160 nM in multi-drug resistant strains of Mycobacterium) than isoniazid (MIC50 = 330 nM) and PA-824 (MIC50 = 400 nM). Exhibits in vivo efficacy in acute and established mouse models of Mycobacterium tuberculosis infection. Exhibits low to moderate metabolic clearance in mouse and human hepatic microsomes. Suggested to inhibit the fatty acid elongation step that blocks the biosynthesis of mycolic acids and weakens the cell wall mycolyl-arabinogalactan-peptidoglycan complex, and ultimately lysis of Mycobacterium.

A cell-permeable, orally available, highly lipophilic 4-hydroxy-2-pyridone derivative that directly binds to the enoyl-substrate binding pocket of Mycobaterial enoyl reductase inhA in an NADH-dependent manner and inhibits its activity (IC50 = 570 nM). Shown to be about 5 to 8 times more potent ((MIC50 = 40 to 160 nM in multi-drug resistant strains of Mycobacterium) than isoniazid (MIC50 = 330 nM) and PA-824 (MIC50 = 400 nM). Exhibits in vivo efficacy in acute and established mouse models of Mycobacterium tuberculosis infection. Exhibits low to moderate metabolic clearance in mouse and human hepatic microsomes. Suggested to inhibit the fatty acid elongation step that blocks the biosynthesis of mycolic acids and weakens the cell wall mycolyl-arabinogalactan-peptidoglycan complex, and ultimately lysis of Mycobacterium.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Primary Target
InhA

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Manjunatha, U., et al. 2015. Sci. Trans. Med.7, 269.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
Protocols & Articles
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