Anti-MRSA agent 46
Anti-MRSA agent 46 is a Methicillin-resistant Staphylococcus aureus (MRSA) membrane-disrupting agent. Anti-MRSA agent 46 disrupts bacterial membrane integrity and morphology, dissipates membrane potential, increases membrane permeability, and perturbs glycerophospholipid metabolism. Anti-MRSA agent 46 induces intracellular DNA and protein leakage, reduces intracellular ATP levels, and induces reactive oxygen species (ROS) production. Anti-MRSA agent 46 disrupts MRSA biofilms, reduces bacterial burden, exhibits a low propensity for resistance, and retains antibacterial activity after plasma exposure, and improves survival in a mouse sepsis infection model. Anti-MRSA agent 46 can be used for research related to MRSA infection.
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- CAS No.: 2883235-38-7
- Formule: C40H64Br2N4O4
- Masse moléculaire:824.77
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
26.21 μg/mL
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Cytotoxicity against mouse NIH/3T3 cells assessed as viability reduction after 24 hrs incubation by CCK-8 assay.
Cytotoxicity against mouse NIH/3T3 cells assessed as viability reduction after 24 hrs incubation by CCK-8 assay.
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42691881 |
| RAW264.7 | IC50 |
17.93 μg/mL
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Cytotoxicity against mouse RAW 264.7 cells assessed as viability reduction after 24 hrs incubation by CCK-8 assay.
Cytotoxicity against mouse RAW 264.7 cells assessed as viability reduction after 24 hrs incubation by CCK-8 assay.
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42691881 |
In Vitro
Anti-MRSA agent 46 (1-8× MIC; 0-8 h) rapidly kills MRSA N315 in both the early and late growth phases[1].
Anti-MRSA agent 46 shows a low propensity for resistance development, with the MIC against MRSA remaining at 1 μg/mL after 20 passages[1].
Anti-MRSA agent 46 (0-6 h) retains anti-MRSA activity after plasma exposure, with an MIC of 2 μg/mL and an MBC of 16 μg/mL[1].
Anti-MRSA agent 46 (1-64 μg/mL; 16-18 h) effectively disrupts preformed MRSA N315 biofilms[1].
Anti-MRSA agent 46 (8 μg/mL; 4 h) disrupts the bacterial envelope morphology of MRSA N315, causing surface collapse and membrane rupture[1].
Anti-MRSA agent 46 (8-32 μg/mL; 0-30 min) dissipates the membrane potential of MRSA N315 in a concentration-dependent manner[1].
Anti-MRSA agent 46 (8-32 μg/mL; 0-30 min) increases MRSA N315 membrane permeability in a time- and concentration-dependent manner[1].
Anti-MRSA agent 46 (8× MIC; 4 h) impairs MRSA N315 membrane integrity, as evidenced by increased PI-positive staining[1].
Anti-MRSA agent 46 (1-8 μg/mL; 4 h) causes leakage of proteins and DNA from MRSA N315[1].
Anti-MRSA agent 46 (1 h) shows no significant hemolytic activity against MRSA N315 at 32× MIC[1].
Anti-MRSA agent 46 (24 h) shows attenuated antibacterial activity in the presence of PG and PE, supporting its preferential interaction with membrane phospholipids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 and NIH/3T3 cells
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Concentration:2, 4, 8, 16, 32 and 64 μg/mL
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Incubation Time:24 h
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Result:Moderate cytotoxicity was observed toward NIH/3T3 and RAW 264.7 cells, with IC50 values of 26.21 and 17.93 μg/mL, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:intraperitoneally; once at 1 h post-infection
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Result:Increased survival to 83.3% at 5 mg/kg and 100% at 10 mg/kg.
Also markedly reduced bacterial burdens in the heart, liver, spleen, lung, and kidney.
Alleviated infection-associated liver and kidney lesions, including vacuolar degeneration and cellular swelling.
Chemical Information
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CAS No. 2883235-38-7
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Masse moléculaire 824.77
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Formule C40H64Br2N4O4
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SMILES
CCCCCNC(C[N+](C)(C)CCOC1=CC=C(C2=C(OCC[N+](C)(C)CC(NCCCCC)=O)C=CC(CC=C)=C2)C=C1CC=C)=O.[Br-].[Br-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anti-MRSA agent 46 Related Classifications
HY-189732 Related Classifications
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