化合物 Metallo-β-lactamase-IN-6 T60239

Product Introduction
Bioactivity


英文名: Metallo-β-lactamase-IN-6

描述: Metallo-β-lactamase-IN-6 is a highly effective inhibitor of VIM-Type metallo-β-lactamase, demonstrating IC 50 values of 0.56 μM, 29.50 μM, and 5.78 μM for VIM-2, VIM-1, and VIM-5, respectively. In addition, Metallo-β-lactamase-IN-6 exhibits potent synergistic antibacterial properties when combined with Meropenem, particularly against engineered Escherichia coli strains and clinically isolated Pseudomonas aeruginosa carrying the VIM-2 MBL gene [1].

体外活性: 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].

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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