BB-3497
BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research.
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- CAS. Nr.: 235784-88-0
- Formel: C16H31N3O4
- Molecular Weight:329.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
BB-3497 binds to PDF such that the oxygen atoms of its N-formyl-hydroxylamine group occupy the positions of the two Ni-bound water molecules observed in the PDF-Met-Ala-Ser product complex[1].
BB-3497 shows superior in vitro antibacterial activity against E. coli DH5α and E. coli BL21(DE3) strains harboring a control plasmid (pET24) or pET24-PDF, with MIC values of 4, 8, 32, and 128 μg/mL, but shows an MIC of >128 μg/mL against an E. coli formyltransferase mutant, confirming that its antibacterial action is mediated through PDF inhibition[1].
BB-3497 (4-8x MIC, 24 h) results in <1-log-unit decreases in viable counts of S. aureus and E. coli, conforming its antibacterial effect[1].
BB-3497 (2-4x MIC, 24 h) results in resistant mutants at frequencies of 1 x 10-7 for E. coli and 2 x 10-7 for S. aureus, with high-level resistance conferred by mutations in the fmt gene and low-level resistance exhibited by mutants having a wild-type def-fmt operon[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUC0-24 |
|---|---|---|---|---|
| Rat[1] | 100 mg/kg | p.o. | 24 mg/L | 34 mg·h/L |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR-derived mice intraperitoneally inoculated with S. aureus[1]
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Dosage:3, 6, 10, 30, 60 and 100 mg/kg
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Administration:p.o. or i.v., single dose at 1 h after bacterial challenge
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Result:Rescued mice from infection with an ED50 of 7 mg/kg (i.v.) and 8 mg/kg (p.o.), respectively.
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Animal Model:Male ICR-derived mice intraperitoneally inoculated with methicillin-resistant S. aureus[1]
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Dosage:3, 6, 10, 30, 60 and 100 mg/kg
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Administration:p.o., single dose at 1 h after bacterial challenge
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Result:Showed an ED50 of 14 mg/kg.
Chemical Information
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CAS. Nr. 235784-88-0
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Molecular Weight 329.44
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Formel C16H31N3O4
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SMILES
CCCC[C@@H](C(N[C@@H](C(C)(C)C)C(N(C)C)=O)=O)CN(O)C=O
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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)
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