Antibacterial agent 237

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Antibacterial agent 237 (compound Ru-8) is a bacteriostatic agent for Staphylococcus aureus, with MIC of 0.78-1.56 μg/mL. Antibacterial agent 237 destroys bacterial cell membranes, changes their permeability, and induces bacteria to produce Reactive Oxygen Species, leading to bacterial death without causing drug resistance. Antibacterial agent 237 has low hemolytic toxicity to rabbit red blood cells and Raw 264.7 cells, and has significant antibacterial effects against Staphylococcus aureus in mouse skin wound infection models and Bacillus major larvae infection models.

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Antibacterial agent 237 Chemical Structure

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Biological Activity
Purity & Documentation
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Description

In Vitro

Antibacterial agent 237 has antibacterial effects on S. aureus Newman, S. aureus ATCC 29213, Methicillin-resistant S. aureus ATCC 33591, E. coli 25922, and PAO1, with MICs of 0.78 μg/mL, 1.56 μg/mL, 1.56 μg/mL, 100 μg/mL, and 50 μg/mL^[1].
Antibacterial agent 237 still maintains the activity of inhibiting S. aureus Newman at high salt concentrations, with a MIC of 0.78 μg/mL, and remains stable in mammalian body fluids (serum, plasma and blood) ^[1].
Antibacterial agent 237 (0-4.68 μg/mL, 0-120 min) can kill S. aureus Newman efficiently and quickly, and is concentration-dependent, effectively avoiding the development of drug resistance^[1].
Antibacterial agent 237 (0-49.92 μg/mL, 24 h) can remove S. aureus Newman biofilms in a dose-dependent manner^[1].
Antibacterial agent 237 (0.39 μg/mL, 5-6 h) is not likely to induce S. aureus Newman resistance^[1].
Antibacterial agent 237 (0.78-4.68 μg/mL, 0-6 h) destroys S. aureus Newman cell membranes, produces ROS, causes bacterial contents to leak, and leads to bacterial death^[1].
Antibacterial agent 237 (0-100 μg/mL, 24 h) has a killing effect on S. aureus Newman and does not damage normal cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	S. aureus Newman
Concentration:	0, 1.56, 3.12, 4.68 μg/mL; 0, 0.78, 1.56, 3.12, 6.24, 12.48, 24.96, 49.92 μg/mL; 0.39 μg/mL; 0.78, 1.56, 3.12, 4.68 μg/mL; 0-100 μg/mL
Incubation Time:	0, 30, 60, 90, 120 min; 24 h; 5-6 h; 0-6 h
Result:	Killed S. aureus Newman within 2 hours at a concentration of 6 × MIC. Did not significantly remove the biofilm at 1 × MIC (0.78 μg/mL), whereas when the concentration increased to 16 × MIC (12.48 μg/mL), the biofilm removal effect decreased by 60%. Did not change the sensitivity of S. aureus Newman and showed no obvious resistance to other antibiotics. Disrupted the cell membrane, causing ROS to accumulate.

Cell Cytotoxicity Assay^[1]

Cell Line:	RAW 264.7
Concentration:	0, 6.25, 12.5, 25, 50, 100 μg/mL
Incubation Time:	24 h
Result:	Had a killing effect on bacteria without damaging normal cells and had good biocompatibility.

Immunofluorescence^[1]

Cell Line:	S. aureus Newman
Concentration:	4.68 μg/mL
Incubation Time:	2 h
Result:	Showed strong red fluorescence, indicating that it had the ability to destroy bacterial cell membranes and had a concentration-dependent depolarization.

In Vivo

Antibacterial agent 237 (0-256 mg/kg, injected at the second pair of ventral pedicles of the tail) showed good drug safety in the C. aureus larvae model and had a good therapeutic effect on C. aureus larvae infection in vivo^[1].
Antibacterial agent 237 (50, 100 μg/mL, applied with sterile cream) has a good therapeutic effect on the mouse model of S. aureus Newman infection^[1].

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

Animal Model:	Large wax borer larvae; G. mellonella larvae model^[1]
Dosage:	0, 32, 64, 128, 256 mg/kg; 128, 256 mg/kg
Administration:	Inject at the second pair of abdominal feet in the tail
Result:	Showed concentration was 32 mg/kg, the survival rate of the larvae of Bacillus waxii was 100%, and even when it was increased to 256 mg/kg, the survival rate of the larvae of Bacillus waxii was still 75%. Showed concentration was 128 mg/kg, the survival rate of the larvae of Bacillus waxii was 75%, and when the dose was increased to 256 mg/kg, the survival rate of the larvae of Bacillus waxii increased by 10%.

Animal Model:	A mouse back wound infection model^[1]
Dosage:	50 and 100 μg/mL
Administration:	Apply
Result:	Healed wounds and reduced bacterial content in wounds.

Molecular Weight

1261.87

Formula

C₆₅H₆₉Cl₃N₁₀RuS₂

SMILES

CC(C)(C)C(C=C1)=CC(C2=CC(C(C)(C)C)=CC=[N]23)=[N]1[Ru+2]435([N]6=CC=CC7=C6C([N]5=CC=C8)=C8C9=C7NC(C%10=CC=C(SC%11=NC(C%12=CC=[N+](CC)C=C%12)=CS%11)C=C%10)=N9)[N]%13=CC=C(C(C)(C)C)C=C%13C%14=[N]4C=CC(C(C)(C)C)=C%14.[Cl-].[Cl-].[Cl-]

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

Handling Instructions (2659 KB)

References

[1]. Wei Deng , et al. Discovery of quaternized pyridine-thiazole-ruthenium complexes as potent anti-Staphylococcus aureus agents. Eur J Med Chem. 2024 Nov 5:277:116712. [Content Brief]