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^[1].

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 (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 T_1/2 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].

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

203.20

C₁₀H₉N₃O₂

1439899-44-1

O=C(C1=NC=CN1CC2=CC=NC=C2)O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Yan YH, Li W, Chen W, et al. Structure-guided optimization of 1H-imidazole-2-carboxylic acid derivatives affording potent VIM-Type metallo-β-lactamase inhibitors. Eur J Med Chem. 2022;228:113965.  [Content Brief]