2. Anti-infection
  3. Beta-lactamase Bacterial
  4. Metallo-β-lactamase-IN-6

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 具有较强的协同抗菌活性，能抑制重组大肠杆菌 (Escherichia coli) 以及临床分离、能产生 VIM-2 MBL 的铜绿假单胞菌 (Pseudomonas aeruginosa)。

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Metallo-β-lactamase-IN-6 Chemical Structure

Metallo-β-lactamase-IN-6 Chemical Structure

CAS No. : 1439899-44-1

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Metallo-β-lactamase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(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.

Metallo-β-lactamase-IN-6 相关抗体:
体内研究
(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.
分子量

203.20

Formula

C10H9N3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Metallo-β-lactamase-IN-6 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Metallo-β-lactamase-IN-61439899-44-1Beta-lactamaseBacterialβ-lactamaseMetallo-β-lactamaseVIMMeropenemSynergistic antibacterial activityEscherichia coliPseudomonas aeruginosaICR miceInhibitorinhibitorinhibit

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