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  3. Metallo-β-lactamase-IN-6

Metallo-β-lactamase-IN-6 

Cat. No.: HY-143414
Handling Instructions

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.

Metallo-β-lactamase-IN-6 Chemical Structure

Metallo-β-lactamase-IN-6 Chemical Structure

CAS No. : 1439899-44-1

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Description

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[1].

IC50 & Target

IC50: 0.56 μM (VIM-2), 29.50 μM (VIM-1), 5.78 μM (VIM-5)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Metallo-β-lactamase-IN-6 (100 mg/kg; IP; single) reaches plasma concentration peak about 9 min after injection with an effective maximum concentration of 142.8 μg/ml, and the T1/2 is 1.24 hours[1].
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female ICR mice (180-220 g)[1]
Dosage: 100 mg/kg
Administration: IP; single (Pharmacokinetics Analysis)
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.
Animal Model: Female ICR mice (n=5)[1]
Dosage: 500, 1000, or 2000 mg/kg
Administration: IP; single, observed for 14 days
Result: Did not result in any significant toxic effects and was well-tolerated by mice at a dose of ≤ 2000 mg/kg.
Molecular Weight

203.20

Formula

C10H9N3O2

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Metallo-β-lactamase-IN-6
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HY-143414
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