Antibacterial agent 340
Antibacterial agent 340 is a DNA gyrase inhibitor. Antibacterial agent 340 exhibits broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria. Antibacterial agent 340 disrupts bacterial cell membrane integrity, induces reactive oxygen species (ROS) accumulation, and inhibits and eradicates bacterial biofilms. Antibacterial agent 340 can be used for the research of bacterial infections.
For research use only. We do not sell to patients.
- Formula: C19H15N3O7
- Molecular Weight:397.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Antibacterial agent 340 (Compound IN 6a) (24 h) potently inhibits growth of Gram-positive bacterial strains with MIC values of 0.03 μg/mL (MRSA) and 0.25 μg/mL (all other strains)[1].
Antibacterial agent 340 (24 h) potently inhibits growth of Gram-negative bacterial strains with MIC values of 0.06 μg/mL (Klebsiella pneumoniae) and 0.25 μg/mL (all other non-P. aeruginosa strains), while showing reduced activity against P. aeruginosa strains with MIC values of 32 to 128 μg/mL[1].
Antibacterial agent 340 exhibits low cytotoxicity against HUVEC cells[1].
Antibacterial agent 340 (2 h) exhibits low hemolytic activity against human erythrocytes, with hemolysis rates below 5% even at a concentration of 256× MIC after 2 h of incubation[1].
Antibacterial agent 340 has a low propensity to induce resistance in MRSA and Klebsiella pneumoniae, with stable MIC values maintained over 24-30 generations[1].
Antibacterial agent 340 exhibits sustained inhibitory activity and low cross-resistance against Norfloxacin (HY-B0132)-, Ciprofloxacin (HY-B0356)-, Cefdinir (HY-B0136)-, and multidrug-resistant MRSA, as well as Norfloxacin-, Ciprofloxacin-, Cefixime-, and multidrug-resistant Klebsiella pneumoniae, with low MIC values maintained for at least 20 generations[1].
Antibacterial agent 340 (24 小时) inhibits biofilm formation in MRSA and Klebsiella pneumoniae in a concentration-dependent manner[1].
Antibacterial agent 340 eradicates pre-formed biofilms in MRSA and Klebsiella pneumoniae in a concentration-dependent manner[1].
Antibacterial agent 340 (60 min) induces membrane depolarization in MRSA and Klebsiella pneumoniae[1].
Antibacterial agent 340 (180 min) increases outer membrane permeability in Klebsiella pneumoniae, but does not affect the outer membrane permeability of Pseudomonas aeruginosa ATCC 9027[1].
Antibacterial agent 340 (6 h) increases inner membrane permeability in MRSA and Klebsiella pneumoniae in a concentration-dependent manner[1].
Antibacterial agent 340 (0.133 mg/kg) provides superior in vivo protection against MRSA infection in Galleria mellonella larvae, resulting in an 80% survival rate on day four post-treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz | CL | MRT0-t | MRT0-∞ | F | C0 |
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| Mice[1] | 10 mg/kg | i.v. | 0.82 h | 0.033 h | 341 ng/mL | 82.3 ng·h/mL | 84.1 ng·h/mL | 6961 mL/kg | 11907 mL/h/kg | 0.49 h | 0.59 h | / | 680 ng/mL |
| Mice[1] | 1 mg/kg | p.o. | 1.23 h | 0.25 h | 19.2 ng/mL | 28.4 ng·h/mL | 29.1 ng·h/mL | 626272 mL/kg | 348155 mL/h/kg | 1.59 h | 1.83 h | 3.46 % | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (female; 7-week-old; 20-25 g)[1]
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Dosage:1 mg/kg (p.o.); 10 mg/kg (i.v.)
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Administration:i.v. or p.o.; single dose
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Result:Exhibited T1/2 of 0.82 h, Tmax of 0.033 h, Cmax of 341 ng/mL, AUC0-t of 82.3 ng·h/mL, AUC0-∞ of 84.1 ng·h/mL, VZ of 6961 mL/kg, CL of 11907 mL/h/kg, MRT0-t of 0.49 h and MRT0-∞ of 0.59 h at 10 mg/kg (i.v.).
Exhibited T1/2 of 1.23 h, Tmax of 0.25 h, Cmax of 19.2 ng/mL, AUC0-t of 28.4 ng·h/mL, AUC0-∞ of 29.1 ng·h/mL, VZ of 626272 mL/kg, CL of 348155 mL/h/kg, MRT0-t of 1.59 h and MRT0-∞ of 1.83 h at 1 mg/kg (p.o.).
Exhibited a poor oral bioavailability of 3.46% (p.o.).
Chemical Information
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Molecular Weight 397.34
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Formula C19H15N3O7
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SMILES
CC1=CC(OC2=C1C=CC(OCC(N/N=C/C=C/C3=CC=C(O3)[N+]([O-])=O)=O)=C2)=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)
Antibacterial agent 340 Related Classifications
HY-183275 Related Classifications
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- Antibacterial agent 340
- Antibacterial agent340
- Antibacterial agent-340
- DNA/RNA Synthesis
- Bacterial
- Reactive Oxygen Species (ROS)
- HUVEC cells
- reactive oxygen species
- MRSA
- Galleria mellonella larvae
- DNA gyrase
- bacterial biofilms
- Klebsiella pneumoniae
- Gram-negative bacteria
- bacterial cell membrane
- Gram-positive bacteria
- Inhibitor
- inhibitor
- inhibit