Metallo-β-lactamase-IN-6
Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL.
For research use only. We do not sell to patients.
- CAS No.: 1439899-44-1
- Formula: C10H9N3O2
- Molecular Weight:203.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 0.56 μM (VIM-2), 29.50 μM (VIM-1), 5.78 μM (VIM-5)[1]
Metallo-β-lactamase-IN-6 (compound 55) (10 μM; 18 - 20 hours) can potentiate Meropenem activity against VIM-2 mediated antibacterial resistance with FIC index values of 0.05[1].
Metallo-β-lactamase-IN-6 (1, 10, 100 μM; 18 - 20 hours) can penetrate E. coli outer membrane and restore Meropenem activity against PBP3 by blocking destructive effect of VIM-2 enzyme to Meropenem[1].
Metallo-β-lactamase-IN-6 (100 μM) potentiates the antibacterial activity of Meropenem against PA W35 with FIC index values of 0.25[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Metallo-β-lactamase-IN-6 (500, 1000, or 2000 mg/kg; IP; single, observe for 14 days) does not result in any significant toxic effects and is well-tolerated by mice at a dose of ≤ 2000 mg/kg[1].
Pharmacokinetic Parameters of Metallo-β-lactamase-IN-6 in male female ICR mice[1].
| IP (100 mg/kg) | |
| T1/2 (h) | 1.243 |
| Cmax (μg/mL) | 142.8 |
| Tmax (h) | 0.151 |
| Vd (mL/kg) | 535.804 |
| CL (mL/h/kg) | 248.512 |
| AUC0-∞ (μg/mL·h) | 896 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female ICR mice (180-220 g)[1]
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Dosage:100 mg/kg
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Administration:IP; single (Pharmacokinetics Analysis)
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Result:Plasma concentration reached its peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 was 1.24 hours.
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Animal Model:Female ICR mice (n=5)[1]
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Dosage:500, 1000, or 2000 mg/kg
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Administration:IP; single, observed for 14 days
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Result:Did not result in any significant toxic effects and was well-tolerated by mice at a dose of ≤ 2000 mg/kg.
Chemical Information
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CAS No. 1439899-44-1
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Molecular Weight 203.20
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Formula C10H9N3O2
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SMILES
O=C(C1=NC=CN1CC2=CC=NC=C2)O
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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)
Metallo-β-lactamase-IN-6 Related Classifications
HY-143414 Related Classifications
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