Antimicrobial agent-54
Antimicrobial agent-54 is a ciprofloxacin-derived multi-target antimicrobial agent that inhibits E. coli DNA gyrase, S. aureus topoisomerase IV, LpxC and urease with IC50 values of 0.182, 3.501, 0.052 and 6.254 μM, respectively. The MIC of Antimicrobial agent-54 against E. coli ATCC 8739 is 0.20 μM. Antimicrobial agent-54 interferes with bacterial cell division, causes transient membrane disruption in Gram-positive bacteria, and induces aberrant penicillin-binding protein activity in Gram-negative bacteria. Antimicrobial agent-54 can be used in the research of bacterial infections, including multidrug-resistant bacterial infections and mycobacterial infections.
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- 화학식: C26H26FN5O5
- 분자량:507.51
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
DNA gyrase 0.182 μM (IC50, E. coli) |
topoisomerase IV 3.501 μM (IC50, S. aureus) |
LpxC 0.052 μM (IC50) |
urease 6.254 μM (IC50) |
Antimicrobial agent-54 (compound 10b) inhibits the growth of E. coli ATCC 8739 (MIC = 0.20 μM) in vitro[1].
Antimicrobial agent-54 activates the SOS DNA damage response in Bacillus subtilis UG10, which is evidenced by the formation of RecA aggregates[1].
Antimicrobial agent-54 induces cell elongation, nucleoid condensation, nucleoid-free regions and abnormal cell branching in E. coli W3110, a phenotype consistent with topoisomerase inhibition and potential impairment of penicillin-binding protein function[1].
Antimicrobial agent-54 potently inhibits E. coli DNA gyrase (IC50 = 0.18 μM) and S. aureus topoisomerase IV (IC50 = 3.501 μM), while exhibits low activity against human topoisomerase II (IC50 = 48.05 μM), showing excellent selectivity[1].
Antimicrobial agent-54 potently inhibits nickel-dependent urease with an IC50 value of 6.254 μM[1].
Antimicrobial agent-54 potently inhibits E. coli LpxC with an IC50 value of 0.052 μM[1].
Antimicrobial agent-54 (20 days) exhibits extremely low potential for resistance development against E. coli NCTC 13476 over 20 days, with only a slight increase in its MIC[1].
Antimicrobial agent-54 exhibits low cytotoxicity against human SH-SY5Y (IC50 = 49.62 μM) and WI-38 (IC50 = 59.35 μM) cells, with a favorable selectivity index of 17[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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분자량 507.51
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화학식 C26H26FN5O5
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SMILES
O=C1C(C(NCC(NO)=O)=O)=CN(C2CC2)C3=C1C=C(F)C(N4CCN(C(C5=CC=CC=C5)=O)CC4)=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antimicrobial agent-54
- Antimicrobial agent54
- Antimicrobial agent 54
- Antibiotic
- Bacterial
- Topoisomerase
- Urease
- H. pylori ATCC 700392
- Gram-negative bacteria
- urease
- mycobacterial species
- E. coli DNA gyrase
- Gram-positive bacteria
- human topoisomerase II
- Bacillus subtilis 2020
- LpxC
- S. aureus topoisomerase IV
- Inhibitor
- inhibitor
- inhibit