Antimicrobial agent-56
Antimicrobial agent-56 is an antimicrobial agent that targets the cell membrane of drug-resistant bacteria. Antimicrobial agent-56 disrupts the cell membrane integrity of methicillin-resistant Staphylococcus aureus (MRSA) via membrane targeting, downregulates lipoteichoic acid biosynthesis and two-component system signaling, inhibits MRSA biofilm formation and eradicates mature biofilms, with a MIC of 6.25 μg/mL. Antimicrobial agent-56 hardly induces drug resistance, exhibits low hemolytic activity, inhibits NO production stimulated by LPS (HY-D1056), and retains the anti-inflammatory activity of Resveratrol (HY-16561). Antimicrobial agent-56 loaded in PVA-SA hydrogel promotes the healing of MRSA-infected wounds and suppresses inflammation. Antimicrobial agent-56 can be used in studies related to MRSA infections.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H41BrN2O4
- Molecular Weight:549.54
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Antimicrobial agent-56 (compound III-5) shows a MIC of 6.25 μg/mL against methicillin-resistant Staphylococcus aureus (MRSA)[1].
Antimicrobial agent-56 (25-50 μg/mL; 2-4 h) exhibits rapid, concentration- and time-dependent bactericidal activity against MRSA[1].
Antimicrobial agent-56 (serially passaged for 15 times, 24 h per passage) consistently maintains an MIC of 6.25 μg/mL against MRSA, with no detectable drug resistance induced [1].
Antimicrobial agent-56 (3.13 μg/mL; 24 h) inhibits MRSA biofilm formation by more than 80%[1].
Antimicrobial agent-56 (50 μg/mL; 24 h) exhibits a clearance rate of over 90% against mature MRSA biofilms pre-incubated for 12 h[1].
Antimicrobial agent-56 (12.5-50 μg/mL; 5 min) induces plasma membrane depolarization in MRSA (detected using the DiSC3-5/SYTOX Green fluorescent probe), with the fluorescence intensity increasing in a concentration-dependent manner, while the control group remains stable[1].
Antimicrobial agent-56 (50 μg/mL; 4 h) treatment results in over 95% PI-positive MRSA as detected by DAPI/PI double staining, indicating disruption of membrane integrity in the vast majority of bacteria, accompanied by dose-dependent leakage of intracellular DNA and proteins[1].
Antimicrobial agent-56 (1.56-25 μg/mL; 24 h) exhibits no significant cytotoxicity against HEK293 human embryonic kidney cells[1].
Antimicrobial agent-56 (25-200 μM; 24 h) exhibits significant cytotoxicity against RAW 264.7 cells at high concentrations, so 50 μM is selected as the safe working concentration for anti-inflammatory experiments[1].
Antimicrobial agent-56 (100-2000 μg/mL; 1 h) shows an HC50 of 843.9 μg/mL and an SI of 135.02 in the hemolysis assay[1].
Antimicrobial agent-56 (50 μM; 18-24 h) significantly inhibits nitric oxide (NO) production in LPS (HY-D1056)-stimulated RAW 264.7 mouse macrophages, retaining the potent anti-inflammatory activity of Resveratrol (HY-16561)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1.56, 3.13, 6.25, 12.5, 25 μg/mL
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity towards HEK293 human embryonic kidney cells.
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Cell Line:RAW 264.7 cells
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Concentration:25, 50, 100, 200 μM
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Incubation Time:24 h
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Result:Exhibited significant cytotoxicity toward RAW 264.7 cells at 100 μM.
50 μM was selected as the safe working concentration for anti-inflammatory experiments.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (KM) mice (female, 4-6 weeks old, weighing 19-22 g)[1]
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Dosage:6.25 mg/kg
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Administration:topical; every other day; 14 days
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Result:Achieved a 96% wound healing rate by day 14.
Reduced residual viable bacteria in the wound tissue significantly compared to the untreated model group.
Reached a 77.95% collagen area fraction in the wound dermis.
Reduced serum levels of TNF-α, IL-6, and IL-1β by 55.49%, 62.72%, and 53.01% respectively relative to the untreated model group.
Showed only minimal scattered inflammatory cell infiltration in the wound dermis.
Exhibited continuous body weight gain throughout the 14-day observation period with no abnormal systemic weight changes.
Presented intact, normal tissue architecture with no detectable toxic pathological alterations in H&E-stained sections of the heart, liver, spleen, lungs, and kidneys.
Chemical Information
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Molecular Weight 549.54
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Formel C28H41BrN2O4
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SMILES
C[N+](C)(CC(NCCCCCC)=O)CCCCOC1=CC=C(/C=C/C2=CC(O)=CC(O)=C2)C=C1.[Br-]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Antimicrobial agent-56 Related Classifications
HY-189221 Related Classifications
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Keywords
- Antimicrobial agent-56
- Antimicrobial agent56
- Antimicrobial agent 56
- Bacterial
- MRSA
- PVA-SA hydrogel
- Gram-positive bacterial cell walls
- murine MRSA-infected wound model
- pro-inflammatory cytokine
- biofilm formation
- teichoic acid biosynthesis pathway
- nitric oxide
- lipoteichoic acid biosynthesis
- bacterial two-component system
- Inhibitor
- inhibitor
- inhibit