Antibacterial agent 358
Antibacterial agent 358 is an antibacterial agent. Antibacterial agent 358 selectively interacts with PG on bacterial cell membranes, causing membrane damage. Antibacterial agent 358 induces bacterial cell membrane depolarization, increased membrane permeability and leakage of intracellular components. Antibacterial agent 358 inhibits biofilm formation and disrupts established biofilms. Antibacterial agent 358 reduces bacterial load and alleviates tissue inflammation in a mouse skin abscess model. Antibacterial agent 358 can be used in research related to Gram-positive bacterial infections and skin abscesses.
For research use only. We do not sell to patients.
- Formula: C31H41Br2N3O
- Molecular Weight:631.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Antibacterial agent 358 (Compound 9c) potently inhibits the growth of Gram-positive bacteria (MIC = 0.5-1 μg/mL) and moderately inhibits Gram-negative bacteria (MIC = 4-16 μg/mL)[1].
Antibacterial agent 358 (0-6 h) exhibits excellent plasma stability and retains bactericidal activity against S. aureus ATCC25923 in mammalian physiological body fluids[1].
Antibacterial agent 358 (1-8 μg/mL; 24 h) exhibits rapid, concentration-dependent bactericidal activity against *Staphylococcus aureus* ATCC25923, achieving complete eradication at 8× MIC within 8 h[1].
Antibacterial agent 358 (0.5-16 μg/mL; 24 h) inhibits biofilm formation of *Staphylococcus aureus* ATCC25923 and partially disrupts mature biofilms in a concentration-dependent manner[1].
Antibacterial agent 358 (0-64 μg/mL) selectively interacts with phosphatidylglycerol (PG) in bacterial cell membranes, with a KD value of 48.8 μM, and this property mediates its selective antibacterial activity[1].
Antibacterial agent 358 (0-64 μg/mL) preferentially alters the ζ-potential of the cell membrane of *S. aureus* ATCC25923 without affecting the surface properties of HEK293T mammalian cells, indicating that it exhibits selective bacterial membrane-disrupting activity[1].
Antibacterial agent 358 disrupts the membrane integrity of *Staphylococcus aureus* ATCC25923, allowing propidium iodide to enter the bacterial cells, thus confirming its membrane-damaging effect[1].
Antibacterial agent 358 (1-8 μg/mL; 20 min) effectively depolarizes and permeabilizes the cytoplasmic membrane of *Staphylococcus aureus* ATCC25923 in a concentration-dependent manner[1].
Antibacterial agent 358 (2.5-1280 μg/mL; 1 h) exhibits low hemolytic activity against mature erythrocytes, with an HC50 of 482.4 μg/mL[1].
Antibacterial agent 358 (1-128 μg/mL; 24 h) exhibits low cytotoxicity against LO2 hepatocytes, with a CC50 of 32.92 μg/mL, and its selectivity index against Gram-positive bacteria reaches 32.92[1].
Antibacterial agent 358 (2-16 μg/mL) induces dose-dependent intracellular ROS production in *Staphylococcus aureus* ATCC25923, which leads to bacterial cell death and induces leakage of intracellular DNA and proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LO2 hepatocytes
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Concentration:1, 2, 4, 8, 16, 32, 64, 128 μg/mL
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Incubation Time:24 h
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Result:Showed low cytotoxicity, with a CC50 (concentration causing 50% cell death) of 32.92 μg/mL.
Maintained cell viability at 71.04% at 16 μg/mL, a concentration exceeding its MIC against Gram-positive bacteria.
Achieved a selectivity index (SI = CC50/MIC) of 32.92 for both S. aureus ATCC25923 and MRSA ATCC43300.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 6-8 weeks old, 18-22 g, SPF, subcutaneous injection of Staphylococcus aureus inoculum to induce skin abscess)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:s.c.; single dose
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Result:Reduced bacterial load in infected skin by 1.86 log units (98.7% bacterial killing) and decreased circulating TNF-α by 84.61 pg/mL and IL-6 by 74.43 pg/mL compared to the vehicle control.
Reduced bacterial load by approximately 3.0 log10 units (99.9% bacterial killing), decreased circulating TNF-α by 120.83 pg/mL and IL-6 by 105.02 pg/mL compared to the vehicle control, and attenuated inflammatory cell infiltration to levels comparable to uninfected control mice.
Showed superior efficacy to vancomycin at an equivalent dose, which achieved a 2.17 log10 reduction (99.3% bacterial killing).
Chemical Information
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Molecular Weight 631.48
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Formula C31H41Br2N3O
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SMILES
O=C(NC1=CC=[N+](CCCCCC)C=C1)/C=C/C2=CC=C(C3=CC=[N+](CCCCCC)C=C3)C=C2.[Br-].[Br-]
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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)
- Antibacterial agent 358
- Antibacterial agent358
- Antibacterial agent-358
- Bacterial
- Reactive Oxygen Species (ROS)
- Gram-positive pathogens
- Gram-negative bacteria
- LO2 hepatocytes
- phosphatidylglycerol
- mature erythrocytes
- Gram-positive bacterial infections
- murine skin abscess model
- biofilm
- S. aureus ATCC25923
- HEK293T
- Inhibitor
- inhibitor
- inhibit