1. Anti-infection
  2. Bacterial
  3. 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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Antimicrobial agent-34 Chemical Structure

Antimicrobial agent-34 Chemical Structure

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Description

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[1].

In Vitro

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.

Cell Viability Assay[1]

Cell Line: Staphylococcus aureus ATCC43300
Concentration: 2, 4, 8, 16 mg/mL
Incubation Time: 0, 2, 4, 6, 8, 10, 12, 20, 24 h
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.

Cell Viability Assay[1]

Cell Line: Staphylococcus aureus ATCC43300
Concentration: 2, 4, 8, 16, 32, 64 mg/mL
Incubation Time: 20 days
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%.
In Vivo

Antimicrobial agent-34 (5 and 10 mg/kg, i.p., continuously at 12-h intervals for 2 days) has a strong inhibitory effect on Gram-positive bacteria in vivo, significantly reducing the bacterial load in the blood, liver, kidney, spleen and other organs of mice in the sepsis model of mice infected with Staphylococcus aureus ATCC43300. TNF-α and IL-6 in the blood of mice are reduced after treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse sepsis model infected by S. aureus ATCC43300[1].
Dosage: 5 and 10 mg/kg; continuously at 12-h intervals for 2 days
Administration: Intraperitoneal injection (i.p.)
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.
Molecular Weight

512.77

Formula

C32H52N2O3

SMILES

CC(C=C1)(CC/C=C(C)\C)OC2=C1C(OCCCNCCCN(CCCC)CCCC)=C(C(C)=O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Antimicrobial agent-34 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Antimicrobial agent-34
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HY-161988
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