Fabimycin
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo.
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- CAS No.: 2651965-71-6
- Formule: C23H25ClN4O3
- Masse moléculaire:440.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
In Vitro
Fabimycin shows outstanding activity against S. aureus (MIC: 4 ng/mL), E. coli MG1655 (MIC: 2 μg/mL)[1].
Fabimycin (4 μg/mL) inhibits 90% of the strainsagainst a panel of 100 K. pneumoniae clinical isolates[1].
Fabimycin enhances the stability of the enzyme-inhibitor complex significantly more than the less active enantiomer in both E. coli and A. baumannii versions of FabI[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Fabimycin (intraperitoneal injection) is tolerated in mice with an MTD of >200 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute pneumonia murine or neutropenic mouse thigh infection model, initiated in CD-1 mice with A. baumannii[1]
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Dosage:50 mg/kg
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Administration:Intramuscular injection, 4, 23, and 41 h postinfection (pneumonia model), or 2, 6, and 11 h postinfection (thigh infection)
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Result:Achieved a >3‑fold decrease in log(CFU/lung) and >2-fold decrease log(CFU/thigh) relative to the vehicle.
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Animal Model:Urinary tract infections (UTIs) model (C3H/HeJ mice)[1]
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Dosage:33.3 mg/kg
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Administration:Intravenous injection, three times a day,
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Result:Achieved 3.0, 2.8, 2.9, and 1.9 log10 reductions in bacterial load relative to the vehicle in the spleen, bladder, liver, and kidney tissues, respectively.
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Animal Model:Neutropenic female BALB/c mice infected with drug-resistant A. baumannii (pharmacokinetic assay)[1]
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Dosage:20, 50, 75, 100 mg/kg
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Administration:Intravenous injection, for a single dose
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Result:Pharmacokinetic profile of Fabimycin.
pharmacokinetic property AUClast (h•μg/mL) T1/2 (h) CL (mL/min/kg) Cmax (μg/mL) 100 mg/kg 69.8 1.4 23.5 47.3 75 mg/kg 45.4 1.4 26.9 34.6
Chemical Information
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CAS No. 2651965-71-6
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Masse moléculaire 440.92
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Formule C23H25ClN4O3
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SMILES
O=C(/C=C/C(C=C1CC[C@@H]2[NH3+])=CN=C1NC2=O)N(C)CC(O3)=C(C)C4=C3C=CC=C4.[Cl-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)