Anti-MRSA agent 45
Anti-MRSA agent 45 is a dihydrofolate reductase (DHFR) inhibitor and membrane-disrupting agent. Anti-MRSA agent 45 disrupts MRSA membrane integrity, increases membrane permeability and induces bacterial morphological damage. Anti-MRSA agent 45 exerts rapid, time- and concentration-dependent bactericidal activity against MRSA, and inhibits MRSA biofilm formation. Anti-MRSA agent 45 is applicable to research related to MRSA infection.
For research use only. We do not sell to patients.
- Formula: C18H16FN5
- Molecular Weight:321.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Anti-MRSA agent 45 (Compound A13) (16-18 h) potently inhibits the growth of S. aureus ATCC 29213 (MIC = 0.008 μg/mL). It also inhibits clinical S. aureus isolates (MICs = 0.016-0.063 μg/mL), MRSA-1 and MRSA-2 (MIC = 0.016 μg/mL), as well as other ESKAPE strains, with MIC values ranging from 0.063 to 8 μg/mL for the latter[1].
Anti-MRSA agent 45 (0.008-0.125 μg/mL; 0-24 h) completely inhibits the growth of MRSA-2 within 24 h of incubation at concentrations ≥ 0.016 μg/mL[1].
Anti-MRSA agent 45 (0.016-2 μg/mL; 0-24 h) exhibits rapid, concentration-dependent bactericidal activity against MRSA-2, reducing bacterial counts by up to 6 log10 CFU/mL within 24 h[1].
Anti-MRSA agent 45 (0.002-0.032 μg/mL; 24 h) potently inhibits biofilm formation by MRSA-2, with nearly complete inhibition at the concentration of 1×MIC (0.016 μg/mL)[1].
Anti-MRSA agent 45 (0.25-4 μg/mL; 24 h) eradicates preformed MRSA-2 biofilms, with a maximum eradication rate of approximately 60% at the concentration of 4 μg/mL[1].
Anti-MRSA agent 45 (1-4 μg/mL; 1 h) disrupts the membrane morphology of MRSA-2 in a concentration-dependent manner, causing severe damage at concentrations ≥ 2 μg/mL[1].
Anti-MRSA agent 45 (1-4 μg/mL; 1 h) disrupts the cell membrane integrity of MRSA-2, increases PI uptake and induces cell death at concentrations ≥ 1 μg/mL[1].
Anti-MRSA agent 45 (1-8 μg/mL; 0-1 h) disrupts the membrane polarization of MRSA-2 in a time- and concentration-dependent manner[1].
Anti-MRSA agent 45 (1-8 μg/mL; 0-1 h) increases the membrane permeability of MRSA-2 in a concentration-dependent manner, and significant PI uptake is observed at concentrations ≥ 1 μg/mL[1].
Anti-MRSA agent 45 (0.5-64 μg/mL; 1 h) shows no significant hemolytic activity against sheep red blood cells, with an HC50 > 64 μg/mL[1].
Anti-MRSA agent 45 (24 h) exhibits moderate cytotoxicity against the CaCo-2 (IC50 = 5.347 μg/mL), 293-T (IC50 = 4.704 μg/mL), AML-12 (IC50 = 4.621 μg/mL) and HepG2 (IC50 = 4.092 μg/mL) cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM mice (female, 4-6 weeks old, 20 g)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:s.c.; single dose
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Result:Significantly reduced skin abscess volumes compared to the model, solvent, and TMP (20 mg/kg) groups.
Eliminated discernible abscesses at 10 and 20 mg/kg doses.
Reduced subcutaneous inflammatory cell infiltration with no suppuration at 10 and 20 mg/kg doses.
Significantly reduced MRSA-2 bacterial load in infected skin tissue compared to the model and TMP groups.
Significantly improved MRSA-induced pathological damage to heart, liver, spleen, lung, and kidney.
Caused no significant organ pathological changes except minor congestion and hemorrhage at 10 and 20 mg/kg doses.
Chemical Information
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Molecular Weight 321.35
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Formula C18H16FN5
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SMILES
NC1=C2C3=C(N(CC4=CC(F)=CC=C4C)C=C3)C=CC2=NC(N)=N1
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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)