MCZ-038
MCZ-038 is a thiourea antibiotic with bactericidal activity. MCZ-038 exerts its effects by interfering with the lipid organization or fluidity of bacterial cell membranes. MCZ-038 can be used in studies related to drug-resistant Staphylococcus aureus infections and Vancomycin (HY-B0671)-resistant Enterococcus faecium infections.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 890179-59-6
- Formel: C18H17Cl2N3S
- Molecular Weight:378.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
MCZ-038 (0-100 µg/mL) shows moderate cytotoxicity against Vero, NIH-3T3, and HepG2 cells, with selectivity indices ranging from 2 to 10 relative to its antistaphylococcal activity[1].
MCZ-038 (4-40 µg/mL; 24 h) exhibits concentration-dependent bactericidal activity against S. aureus ATCC 29213, reducing bacterial load by ~4 log10 CFU/mL at 10x MIC (40 µg/mL) over 24 h[1].
MCZ-038 (0.125-16 µg/mL; 18-24 h) exhibits partial synergy with Gentamicin (HY-A0276) against S. aureus ATCC 29213 (ΣFIC 0.625) and a synergistic bactericidal effect in combination with gentamicin against both S. aureus ATCC 29213 and gentamicin-resistant MDR MRSA NRS119[1].
MCZ-038 (4 µg/mL; 24-48 h) eradicates pre-formed S. aureus ATCC 29213 biofilms as effectively as vancomycin[1].
MCZ-038 (4 µg/mL; 24 h) exhibits superior activity against intracellular S. aureus ATCC 29213 in J774A.1 macrophages, reducing bacterial load by ~0.6 log10 CFU/mL at 4 µg/mL over 24 h[1].
MCZ-038 (2 µg/mL; 30 days) shows no propensity to induce resistance in S. aureus ATCC 29213 over 30 days of serial passaging[1].
MCZ-038 (0-64 µg/mL; 10 h) exerts its antimicrobial activity by perturbing bacterial membrane integrity and fluidity, without targeting cell wall, DNA, RNA, or protein biosynthesis, and does not cause unspecific membrane disruption[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MCZ-038 (2% formulation; topical; twice daily; 4 days) reduces gentamicin-resistant MDR MRSA NRS119 burden in murine superficial skin tissue by ~1 log10 CFU/g[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (male, 22-25 g, neutropenic via intraperitoneal cyclophosphamide injections at 150 mg/kg 4 days pre-infection and 100 mg/kg 1 day pre-infection)[1]
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Dosage:50 mg/kg
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Administration:i.p.; two doses at 2 h and 6 h post-infection
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Result:Reduced bacterial burden in thigh tissue by ~0.5 log10 CFU/g.
Reduced bacterial burden in thigh tissue by ~1 log10 CFU/g when combined with gentamicin, which was superior to individual treatments.
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Animal Model:Swiss mice (male, 4-6 weeks old, 22-25 g)[1]
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Dosage:2% formulation
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Administration:topical; twice daily; 4 days
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Result:Reduced bacterial burden in skin tissue by ~1 log10 CFU/g, outperforming gentamicin which did not significantly reduce bacterial load compared to the untreated group.
Chemical Information
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CAS. Nr. 890179-59-6
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Molecular Weight 378.32
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Formel C18H17Cl2N3S
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SMILES
S=C(NC1=CC=C(Cl)C=C1C)NCCC2=CNC3=C2C=C(Cl)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- MCZ-038
- 890179-59-6
- MCZ038
- MCZ 038
- Antibiotic
- Bacterial
- vancomycin-resistant Enterococcus faecium
- CysLT1 receptors
- CysLT2 receptors
- J774A.1 macrophages
- Staphylococcus aureus
- macrophages
- vancomycin-resistant S. aureus
- methicillin-resistant S. aureus
- murine skin infection models
- murine thigh infection models
- Inhibitor
- inhibitor
- inhibit