Antibacterial agent 356
Antibacterial agent 356 is an orally active antibacterial agent. Antibacterial agent 356 binds to the Mrr1 transcription factor, inhibits the expression of the MDR1 efflux pump gene, reduces the efflux of Rhodamine 123, and increases the accumulation of intracellular substrates in drug-resistant Candida albicans cells. Antibacterial agent 356 induces mitochondrial membrane potential reduction and ROS accumulation in Candida albicans, inhibits the yeast-hypha transition process, and suppresses its biofilm formation. Antibacterial agent 356 reverses efflux pump-mediated drug resistance in azole-resistant Candida albicans with overexpressed Mdr1. Antibacterial agent 356 improves the survival rate of Galleria mellonella larvae infected with azole-resistant Candida albicans*CA632, and reduces the renal fungal load and renal tissue damage in infected BALB/c mice. Antibacterial agent 356 can be used for the research of Candida albicans infection.
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- Formule: C14H9F2NO2S
- Masse moléculaire:293.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Antibacterial agent 356 (compound 6AO) exhibits selective in vitro antifungal and antibacterial activity, with potent inhibition of Staphylococcus aureus (MIC 0.4 μM) and moderate activity against Candida albicans and Cryptococcus neoformans, but no activity against Aspergillus fumigatus, Escherichia coli, or Pseudomonas aeruginosa[1].
Antibacterial agent 356 synergizes with multiple azole drugs to reverse azole resistance in Mdr1-overexpressing Candida albicans CA632 and G5, shows additive activity against Cdr1/Cdr2-overexpressing strains, and has no activity against drug-resistant Candida auris[1].
Antibacterial agent 356 (27.3-109.2 μM; 6 h) inhibits efflux pump function in drug-resistant Candida albicans CA632 by downregulating efflux pump gene expression, particularly MDR1, and enhances the suppressive effect of Fluconazole (HY-B0101) on MDR1 expression[1].
Antibacterial agent 356 (13.7-218.4 μM; 24 h) exhibits concentration-dependent antifungal activity against Candida albicans SC5314, with fungicidal effects at 218.4 μM and fungistatic effects at 109.2 μM[1].
Antibacterial agent 356 (54.6-218.4 μM; 3-6 h) induces mitochondrial dysfunction in Candida albicans SC5314, characterized by dose-dependent loss of membrane potential and excessive ROS accumulation at intermediate concentrations[1].
Antibacterial agent 356 (13.7-218.4 μM; 6 h) inhibits yeast-to-hyphal transition in Candida albicans SC5314[1].
Antibacterial agent 356 (54.6-436.8 μM) potently inhibits biofilm formation in Candida albicans SC5314 in a dose-dependent manner[1].
Antibacterial agent 356 (1-100 μM; 48 h) exhibits minimal cytotoxicity against human normal hepatocytes (L02) at concentrations up to 100 μM[1].
Antibacterial agent 356 (24 days) has a low propensity to induce resistance in Candida albicans SC5314[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human normal hepatocytes (L02)
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Concentration:1 μM, 10 μM, 20 μM, 50 μM, 80 μM, 100 μM
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Incubation Time:48 h
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Result:Maintained cell viability above 80% across all tested concentrations, with minimal cytotoxicity relative to the blank group.
Antibacterial agent 356 (5-10 mg/kg; oral gavage; daily; 6 days) reduces kidney fungal burden and renal tissue damage in immunocompromised BALB/c mice infected with azole-resistant C. albicans CA632, with a significantly greater effect observed when combined with 5 mg/kg Fluconazole[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:larvae (~0.25 g, free of melanization)[1]
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Dosage:2400 ng/larvae; 3200 ng/larvae; 3200 ng/larvae + 800 ng/larvae fluconazole
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Administration:intrahemocoel injection; single dose
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Result:Elevated larval survival versus vehicle controls (3200 ng/larvae monotherapy).
Decreased melanized nodule size and count relative to untreated infected groups (3200 ng/larvae monotherapy).
Boosted larval survival and lowered melanized nodule burden far more potently than 3200 ng/larvae monotherapy (3200 ng/larvae + 800 ng/larvae fluconazole combination).
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Animal Model:BALB/c (female, 4-6 weeks old, 18-20 g, cyclophosphamide-induced immunosuppression)[1]
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Dosage:5 mg/kg; 10 mg/kg; 10 mg/kg + 5 mg/kg fluconazole
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Administration:oral gavage; daily; 6 days
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Result:Reduced renal fungal loads relative to vehicle controls (10 mg/kg monotherapy).
Lessened fungal abundance and alleviated fungal-triggered renal lesions versus untreated infected groups (10 mg/kg monotherapy).
Markedly cut renal fungal loads and mitigated renal tissue injury superior to 10 mg/kg monotherapy, with intact, tightly arranged renal tubular epithelia (10 mg/kg + 5 mg/kg fluconazole combination).
Chemical Information
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Masse moléculaire 293.29
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Formule C14H9F2NO2S
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SMILES
FC1=CC(F)=C(C=C1)C(C2=NOC(C2)C3=CC=CS3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antibacterial agent 356 Related Classifications
HY-184587 Related Classifications
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- Antibacterial agent 356
- Antibacterial agent356
- Antibacterial agent-356
- Bacterial
- P-glycoprotein
- Reactive Oxygen Species (ROS)
- Rhodamine 123
- MDR1 efflux pump
- fluconazole
- BALB/c mice
- Staphylococcus aureus
- Candida albicans
- mitochondrial dysfunction
- Mrr1 transcription factor
- biofilm formation
- Galleria mellonella larvae
- Inhibitor
- inhibitor
- inhibit