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Metallo-β-lactamase-IN-6

产品编号 T60239 CAS 1439899-44-1

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].

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Metallo-β-lactamase-IN-6 Chemical Structure

Metallo-β-lactamase-IN-6, CAS 1439899-44-1

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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生物活性

化学信息

存储 & 溶解度

产品描述	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.

分子量	203.2
分子式	C10H9N3O2
CAS No.	1439899-44-1

存储

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

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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