Metallo-β-lactamase-IN-6 是一种有效的VIM型金属 β-内酰胺酶 (metallo-β-lactamase) 抑制剂，对VIM-2、VIM-1和VIM-5 的IC50为 0.56 μM、29.50 μM 和 5.78 μM。Metallo-β-lactamase-IN-6 与 Meropenem 对重组大肠杆菌 (Escherichia coli) 和临床分离的、顽固的、产 VIM-2 MBL 的铜绿假单胞菌 (Pseudomonas aeruginosa)显示出较强的的协同抗菌活性。

Metallo-β-lactamase-IN-6 is a potent VIM -Type metallo-β-lactamase inhibitor with IC 50 s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 shows potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL [1].

Metallo-β-lactamase-IN-6 (compound 55) (10 μM; 18 - 20 hours) can potentiate the activity of Meropenem 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].

Metallo-β-lactamase-IN-6 (100 mg/kg; IP; single) reaches plasma concentration peak approximately 9 min after injection with an effective maximum concentration of 142.8 μg/ml and the T 1/2 of 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) T 1/2 (h) 1.243 C max (μg/mL) 142.8 T max (h) 0.151 Vd (mL/kg) 535.804 CL (mL/h/kg) 248.512 AUC 0-∞ (μg/mL·h) 896 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 T 1/2 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.

1439899-44-1

C10H9N3O2

203.201

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years