2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Topoisomerase DNA/RNA Synthesis
  4. Antibacterial agent 352

Antibacterial agent 352 is an orally active Antibacterial agent. Antibacterial agent 352 binds to the active cavity of Staphylococcus aureus DNA gyrase via hydrogen bonding, π-π stacking and hydrophobic interactions, thereby blocking bacterial DNA synthesis. Antibacterial agent 352 exhibits antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus pumilus, Staphylococcus epidermidis and Enterococcus faecalis. Antibacterial agent 352 can disrupt established Staphylococcus aureus biofilms and inhibit the formation of Staphylococcus aureus biofilms. Antibacterial agent 352 can be used in the research of Staphylococcus aureus wound infections.

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Antibacterial agent 352

Antibacterial agent 352 Chemical Structure

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Antibacterial agent 352 Related Antibodies

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Description

Antibacterial agent 352 is an orally active Antibacterial agent. Antibacterial agent 352 binds to the active cavity of Staphylococcus aureus DNA gyrase via hydrogen bonding, π-π stacking and hydrophobic interactions, thereby blocking bacterial DNA synthesis. Antibacterial agent 352 exhibits antibacterial activity against Gram-positive bacteria including Staphylococcus aureus, Bacillus pumilus, Staphylococcus epidermidis and Enterococcus faecalis. Antibacterial agent 352 can disrupt established Staphylococcus aureus biofilms and inhibit the formation of Staphylococcus aureus biofilms. Antibacterial agent 352 can be used in the research of Staphylococcus aureus wound infections[1].

IC50 & Target[1]

DNA Gyrase

 

In Vitro

Antibacterial agent 352 (Compound W-2-4) (24 h) potently inhibits the growth of S. aureus ATCC 6538 (MIC = 2 μg/mL), B. pumilus AS1.212 (MIC = 2 μg/mL), S. epidermidis ATCC122228 (MIC = 4 μg/mL), and E. faecium AS1.130 (MIC = 0.5 μg/mL) in vitro[1].
Antibacterial agent 352 (1-8 μg/mL; 24 h) acts as a bactericidal agent against S. aureus ATCC 6538 with an MBC of 8 μg/mL (MBC/MIC ratio = 4)[1].
Antibacterial agent 352 (20-400 μg/mL; 3 h) disrupts the membrane integrity of S. aureus ATCC 6538, causing concentration- and time-dependent leakage of intracellular proteins[1].
Antibacterial agent 352 (0.5-8 μg/mL; 24 h) disrupts pre-formed S. aureus ATCC 6538 biofilms in a concentration-dependent manner, achieving a 67.9% clearance rate at 8 μg/mL (4×MIC)[1].
Antibacterial agent 352 (1.2-100.0 μg/mL; 72 h) has low cytotoxicity against HaCaT and H1975 cells, with IC50 values greater than 100 μM, resulting in a selectivity index greater than 19.9 against S. aureus ATCC 6538[1].
Antibacterial agent 352 (8-512 μg/mL; 1 h) exhibits minimal hemolytic activity against sheep erythrocytes, with hemolysis rates below 7% even at concentrations up to 512 μg/mL[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Antibacterial agent 352 Related Antibodies
In Vivo

Antibacterial agent 352 (10-30 mg/kg; p.o.; every other day; administered for a total of 6 times) exhibits dose-dependent in vivo antibacterial efficacy and wound healing activity in a mouse S. aureus wound infection model, achieving complete bacterial clearance and full wound healing at the oral dose of 30 mg/kg[1].
Antibacterial agent 352 (30-60 mg/kg; p.o.; daily; for 7 consecutive days) shows no significant acute systemic toxicity in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KM mice (female, 4-5 weeks old, SPF-grade)[1]
Dosage: 10 mg/kg; 20 mg/kg; 30 mg/kg
Administration: p.o.; every other day; 6 doses
Result: Accelerated wound healing compared to the saline control at 12 days post-treatment.
Reduced bacterial burden in wound tissue by one-log (≈300 CFU at 104 dilution, vs. ≈3000 CFU in the control) at 10 mg/kg dose at 12 days post-treatment.
Achieved a wound healing rate of ≈94.73% (comparable to vancomycin 20 mg/kg) at 20 mg/kg dose at 12 days post-treatment.
Reduced bacterial burden by two-log (17 CFU at 104 dilution) at 20 mg/kg dose at 12 days post-treatment.
Resulted in complete wound healing at 30 mg/kg dose at 12 days post-treatment.
Eradicated all S. aureus from wound tissue (no bacterial colonies recovered) at 30 mg/kg dose at 12 days post-treatment.
Reduced inflammatory cell infiltration, preserved intact tissue structure, and showed regularly arranged collagen fibers (resembling normal tissue) via histopathological analysis at 30 mg/kg dose.
Molecular Weight

437.83

Formula

C22H16ClN3O5
SMILES

O=C(O)CCN(C(C1=CC=C(N/N=C/C2=CC(Cl)=CC=C2O)C3=CC=CC4=C13)=O)C4=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Antibacterial agent 352 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antibacterial agent 352Antibacterial agent352Antibacterial agent-352BacterialTopoisomeraseDNA/RNA Synthesissheep erythrocytesDNA gyraseGram-positive bacteriaH1975 cellsHaCaT cellsStaphylococcus aureusEnterococcus faeciumBacillus pumilusStaphylococcus epidermidisKM miceInhibitorinhibitorinhibit

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