Antimicrobial agent-34
Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300.
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- No. CAS: 3055131-42-2
- Fòrmula: C32H52N2O3
- Peso molecular:512.77
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Antimicrobial agent-34 can be stably present in human serum, plasma and blood, with MBCs of 16, 16 and 32 μg/mL, respectively, without losing its antimicrobial effect[1].
Antimicrobial agent-34 has the strongest antibacterial activity against 6 Gram-positive bacteria, with a wide antibacterial spectrum and a MIC range of 1-4 μg/mL. It also has good antibacterial activity against Klebsiella pneumoniae ATCC10031, Unstable Bacteria ATCC19606, and Escherichia coli ATCC25922, with MICs of 4, 2, and 4 μg/mL, respectively[1].
Antimicrobial agent-34 (1×-16× MIC) shows rapid antibacterial activity against Staphylococcus aureus, and it is dose-dependent[1].
Antimicrobial agent-34 (2-16 mg/mL; 0-24 h) is difficult to induce resistance. The resistance test of Staphylococcus aureus ATCC43300 under sub-MIC (1/2 MIC) shows a MIC change of only 2-4 times[1].
Antimicrobial agent-34 (2-64 mg/mL, 0-20 days) has a strong ability to inhibit biofilm formation and destroy pre-formed biofilm, and it is dose-dependent[1].
Antimicrobial agent-34 (2-32 mg/mL, 0-20 min) disruptes the transmembrane potential of S. aureus, thereby increasing permeability and effectively increasing the levels of ROS, DNA, and protein in S. aureus[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Staphylococcus aureus ATCC43300
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Concentration:2, 4, 8, 16 mg/mL
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Incubation Time:0, 2, 4, 6, 8, 10, 12, 20, 24 h
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Result:Achieved a 8.35 log reduction (killing ≥99.9 % of S. aureus) in 4 h compared with the control, and the killing rate was 100 % after 8 h, while reference drug vancomycin exhibited a 8.55 log reduction of S. aureus within 8 h at the same concentration.
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Cell Line:Staphylococcus aureus ATCC43300
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Concentration:2, 4, 8, 16, 32, 64 mg/mL
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Incubation Time:20 days
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Result:Inhibited the formation of biofilm of Staphylococcus aureus, and the formation of biofilm was significantly reduced with the increase of concentration. 8 μg/mL eliminated 26.69% of the established biofilm of Staphylococcus aureus, and the eradication rate of biofilm at 64 μg/mL exceeded 40%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse sepsis model infected by S. aureus ATCC43300[1].
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Dosage:5 and 10 mg/kg; continuously at 12-h intervals for 2 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Achieved 1.10, 1.98, 2.00 and 2.09 log (91.8 %, 98.9 %, 99.0 % and 99.2 %) reductions in the number of surviving bacterial colonies in blood, liver, spleen and kidney by 5mg/mL.
Achieved, respectively, 1.46, 2.69, 2.24 and 2.84 log (95.9 %, 99.8 %, 99.4 % and 99.9 %) by 10mg/mL.
Decreased in the level of proinflammatory cytokines including TNF-α and IL-6.
Chemical Information
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No. CAS 3055131-42-2
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Peso molecular 512.77
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Fòrmula C32H52N2O3
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SMILES
CC(C=C1)(CC/C=C(C)\C)OC2=C1C(OCCCNCCCN(CCCC)CCCC)=C(C(C)=O)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)