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.
For research use only. We do not sell to patients.
- CAS No.: 1371629-36-5
- Formula: C20H16F2N2O3
- Molecular Weight:370.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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) |
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.
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 No. 1371629-36-5
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Molecular Weight 370.35
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GC-072 Related Classifications
Cat. No.: HY-178738
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- 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