Antibacterial agent 365
Antibacterial agent 365 is a benzothiazole-based antibacterial agent that primarily exerts its effects by disrupting bacterial cell membranes. Antibacterial agent 365 exhibits a MIC of 4 μg/mL against Staphylococcus aureus ATCC 29213, MRSA ATCC BAA41 and MRSA ATCC 43300. Antibacterial agent 365 can be used in studies of MRSA infection, bacterial cell membrane disruption, biofilm formation and antimicrobial resistance.
For research use only. We do not sell to patients.
- Formula: C14H9BrN2O3S
- Molecular Weight:365.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Antibacterial agent 365 (compound 7k) inhibits the growth of S. aureus ATCC 29213, MRSA ATCC BAA41 and MRSA ATCC 43300, with an MIC of 4 μg/mL for all; its MIC against E. coli ATCC 25922 is > 256 μg/mL[1].
Antibacterial agent 365 (0.5-24 h) exhibits concentration- and time-dependent bactericidal activity against S. aureus ATCC 29213; 2 × MIC reduces the bacterial load by nearly 3 log CFU/mL within 24 h, while at 8 h, 2 ×, 4 × and 8 × MIC reduce the bacterial load by 2.64, 2.33 and 3.27 log CFU/mL, respectively[1].
In the drug resistance induction experiment involving 21 consecutive passages of S. aureus ATCC 29213, the MIC of antibacterial agent 365 increases by less than 8-fold, while the MIC of Norfloxacin (HY-B0132) increases by 128-fold, suggesting that it has a moderate tendency to induce drug resistance under these experimental conditions[1].
Antibacterial agent 365 (24 h) inhibits S. aureus ATCC 29213 biofilm formation in a dose-dependent manner, with inhibition rates of 29.21% and 86.84%, respectively[1].
Antibacterial agent 365 (100 or 200 μM; 24 h) exhibits low cytotoxicity against normal human HFF-1 and BJ cells; the cell viability remains close to 100% at 200 μM[1].
Antibacterial agent 365 (200 μM; 1 h) induces a hemolysis rate of 5.13% in human red blood cells[1].
Antibacterial agent 365 increases the fluorescence signal of S. aureus ATCC 29213 in a dose-dependent manner in the SYTOX Green assay, indicating increased bacterial cell membrane permeability and impaired membrane integrity[1].
Antibacterial agent 365 (4 h) renders S. aureus ATCC 29213 PI-positive in SYTO9/PI staining, and induces rough, shrunken and ruptured cell membranes under SEM, which further indicates that it directly damages bacterial cell membranes[1].
Antibacterial agent 365 inhibits S. aureus DNA gyrase mainly at concentrations far higher than its MIC; it shows only approximately 9.3% enzyme inhibition at 100 μM, while the inhibition increases at 200 μM. Therefore, DNA gyrase is not the primary target of its antibacterial action at the MIC level[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HFF-1 (ATCC SCRC-1041), BJ (ATCC CRL-2522)
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Concentration:200 μM
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Incubation Time:24 h
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Result:Maintained 100% cell viability in both HFF-1 and BJ cell lines, with viability comparable to or better than the 1% DMSO control.
Had an MIC against Gram-positive bacteria (10.95 μM) far lower than the 200 μM cytotoxicity test concentration.
Antibacterial agent 365 (0.01, 1, or 100 mg/kg; p.o.; single administration) causes no mortality or obvious toxicity in KM mice within a 14-day observation period; further single intragastric administration at 4000 mg/kg also results in no mortality, clinical manifestations of systemic toxicity, or obvious pathological changes, with an MTD ≥ 4000 mg/kg[1].
Topical application of antibacterial agent 365 (100 mg/mL; 0.5 mL/site; topical patch; 4 h) induces only mild and transient erythema without observable edema in male New Zealand white rabbits, with a PII of 0.17, and it is classified as having negligible skin irritation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand White rabbits (male, 2.25 kg)[1]
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Dosage:100 mg/mL
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Administration:topical; single application; 4 h
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Result:Elicited only very slight and transient erythema at application sites in all three rabbits at 1 and 24 h after administration.
Caused no oedema throughout the study.
Resulted in a mean primary irritation index (PII) of 0.17.
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Animal Model:KM mice (male and female, 6-8 weeks old, 20-25 g)[1]
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Dosage:0.01 mg/kg; 1 mg/kg; 100 mg/kg; 4000 mg/kg
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Administration:p.o.; single dose
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Result:Caused no deaths or treatment-related adverse effects at any dose level over the 14-day monitoring period.
Showed no treatment-related gross pathological changes at the 4000 mg/kg dose.
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Animal Model:BALB/c mice (female, 6-8 weeks old, 18-22 g)[1]
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Dosage:10 mg/kg
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Administration:topical to wound; 5 times over 4 days
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Result:Increased wound healing rate compared to the PBS-treated control group.
Reduced neutrophil cell count and promoted visible collagen deposition compared to the PBS group, as shown by Masson staining.
Lowered bacterial colony number by approximately 0.23 logarithmic CFU/mL relative to the PBS group.
Chemical Information
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Molecular Weight 365.20
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Formula C14H9BrN2O3S
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SMILES
OC1=C(O)C=CC(C(NC2=NC3=C(C=C(Br)C=C3)S2)=O)=C1
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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)
Antibacterial agent 365 Related Classifications
HY-187561 Related Classifications
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