GC-072
GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1371629-36-5
- Formel: C20H16F2N2O3
- Molecular Weight:370.35
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
DNA Gyrase 2 μM (IC50, S. aureus) |
TOPO IV 4-30 μM (IC50, S. aureus) |
DNA Gyrase 0.18-1.5 μM (IC50, E.coli) |
TOPO IV 4.22-8.45 μM (IC50, E.coli) |
In Vitro
GC-072 (0.25 μg/mL, 2.5 μg/mL; 0, 1, 5, 24 hours) effectively inhibits the growth of intracellular B. pseudomallei in murine macrophage cells in a rapid time- and dose-dependent manner, with no viable bacteria detectable after 24 hours at either concentration[1].
GC-072 inhibits both E.coli and S. aureus gyrase and Topo IV. The IC50 values of 2 μM, 0.18-1.50 μM, 4-30 μM, and 4.22-8.45 μM for S. aureus gyrase, E.coli gyrase, S. aureus Topo IV, and E.coli Topo IV, respectively[1].
GC-072 demonstrates good activity against B. pseudomallei, with an MIC90 of 0.25 μg/mL and a range of ≤0.008 to 1 μg/mL[1].
The MIC90s of GC-072 against B. anthracis, Y. pestis, F. tularensis, and B. mallei are 0.002 μg/mL, 0.015 μg/mL, ≤0.0005 μg/mL, and 0.12 μg/mL, respectively[1].
GC-072 is fully active against the panel of drug-resistant B. pseudomallei strains tested (i.e., Ceftazidime (HY-B0593)-, Clavulanate (HY-A0256A)- and Trimethoprim (HY-B0510)-resistant strains)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:oral (gavage); 1, 3, 10, 30 mg/kg; q8h; 14 days
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Result:When treatment was initiated 8 h postchallenge, 0%, 0%, 70%, and 90% survival was observed in mice administered 1, 3, 10, and 30 mg/kg, respectively.
When treatment was initiated 16 h postchallenge, 50% and 100% survival was observed in the 10 and 30 mg/kg groups, respectively.
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Animal Model:BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
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Dosage:37.5 mg/kg, 75 mg/kg, 150 mg/kg
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Administration:oral (gavage); 37.5, 75, 150 mg/kg; q8h; 14 days
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Result:When initiated 8 h postexposure, mice in the 37.5-, 75-, and 150-mg/kg treatment groups demonstrated 90%, 90%, and 80% survival, respectively.
In the 24-h treatment initiation groups, overall survival was low. However, each dose provided a significant survival advantage compared to vehicle control.
Chemical Information
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CAS. Nr. 1371629-36-5
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Molecular Weight 370.35
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Formel C20H16F2N2O3
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SMILES
O=C(C1=CC(C2CC2)=C3C(C)=C(C4=C(F)C=C(N)C(F)=C4)C=CN3C1=O)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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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
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- GC-072
- 1371629-36-5
- GC072
- GC 072
- Antibiotic
- Bacterial
- Topoisomerase
- DNA/RNA Synthesis
- bacterial topoisomerases
- reduced development of resistance
- first-line
- oral treatment
- drug-resistant strains
- melioidosis
- bactericidal
- lethal inhalational models
- 4-oxoquinolizine antibiotic
- oral administration
- potent
- extra- and intracellularly
- selective inhibitory activity
- rapid killing
- dose-dependent survival
- intragastrically
- Inhibitor
- inhibitor
- inhibit