Anti-MRSA agent 20
Anti-MRSA agent 20 (Compound a4) is an anti-microbial agent (MIC: < 0.03125 μg/mL) against MRSA). Anti-MRSA agent 20 binds to the ribosomal peptidyl transferase center and inhibits bacterial survival by inhibiting MRSA toxin synthesis and bacterial division. Anti-MRSA agent 20 significantly reduces the MRSA load in the lungs and attenuates lung injury in the MRSA-infected mice (ED50 = 6.48 mg/kg).
For research use only. We do not sell to patients.
- Formula: C34H47NO8S2
- Molecular Weight:661.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Anti-MRSA agent 20 inhibits the growth of Staphylococcus aureus ATCC 29213, MRSA ATCC 43300 and MRSE ATCC 51625, with a minimum inhibitory concentration (MIC) of less than 0.03125 μg/mL[1].
Anti-MRSA agent 20 (1× MIC-6× MIC, 0-24 h) exhibits inhibitory activity against MRSA in time-kill kinetic experiments[1].
Anti-MRSA 20 (21 days) slows the development of bacterial resistance to it, reaching a MIC of 8 μg/mL on days 17-18[1].
Anti-MRSA agent 20 (LC50 of 165.0 μg/mL) is toxic to HEK293 and HEPG2 cells only in the high concentration range (> 120 μg/mL), and inhibits MRSA toxin synthesis in the low concentration range (0.5-1 μg/mL), and has no significant teratogenic effects on zebrafish embryos[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MRSA
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Concentration:1 × MIC, 3 × MIC, 6 × MIC
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Incubation Time:24 h
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Result:Killed 99.9 % of MRSA at 3 × MIC after 4 h.
Killed 99.99 % of MRSA at 6 × MIC after 12 h.
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Cell Line:HEK293 and HEPG2 cells
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Concentration:7.5, 15, 30, 60, 120, 250 μg/mL
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Incubation Time:6 h
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Result:Showed minor toxicity to HEK293 cells at concentrations up to 120 μg/mL.
Displayed toxicity to HEPG2 cells at a concentration of 250 µg/mL.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MRSA-infected mice[1]
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Dosage:2.5, 5, 10, 20, 40 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Increased survival of mice.
Reduced bacterial load in lungs of mice.
Alleviated MRSA-induced lung lesions such as congestion, hemorrhage and inflammatory cell infiltration.
Chemical Information
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Molecular Weight 661.87
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Formula C34H47NO8S2
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SMILES
O=C(COC1=C(SCC(O[C@H]2[C@](C)([C@H](C)CC3)[C@]([H])(C(CC4)=O)[C@@]34[C@@H](C)[C@H](O)[C@](C)(C=C)C2)=O)C=CC=C1)N(CC5)CCS5(=O)=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)