1. Anti-infection
  2. Beta-lactamase Bacterial
  3. Metallo-β-lactamase-IN-9

Metallo-β-lactamase-IN-9 (Compound 23) 是泛金属-β-内酰胺酶 (MBL) 抑制剂,对 NDM-1VIM-1IMP-1IC50 分别为 35、269 和 369 nM。

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Metallo-β-lactamase-IN-9 Chemical Structure

Metallo-β-lactamase-IN-9 Chemical Structure

CAS No. : 1802363-75-2

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  • 生物活性

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  • 参考文献

生物活性

Metallo-β-lactamase-IN-9 (Compound 23) is a pan metallo-beta-lactamase (MBL) inhibitor with IC50s of 35, 269 and 369 nM against NDM-1, VIM-1 and IMP-1, respectively[1].

IC50 & Target

IC50: 35 nM (NDM-1), 269 nM (VIM-1), 369 nM (IMP-1)[1]

体内研究
(In Vivo)

Metallo-β-lactamase-IN-9 (Compound 23) (10 and 50 mg/kg; s.c.; three times a day for 1 day) 在小鼠 Klebsiella pneumoniae MB9249 感染模型中与 Imipenem (HY-B1369A) 联用减少脾脏和肾脏的细菌负担[1]
Mouse Pharmacokinetic Properties of Metallo-β-lactamase-IN-9 (Compound 23)d[1]

dosea(iv, mpk) AUC (μM·h) MRT (h) Vdss (L/kg) Cl (mL/min/kg)
5a 27.08 5.2 2.97 9.33

dose (sc, mg/kg) AUC (μM·h) Cmax (μM) Tmax (h)
10b 27.42 13.4 0.83
50c 111.28 69.1 0.5

aFormulation, 1.0 mg/mL 23 in 20% DMSO/60% PEG400/20% water (solution) with dose volume of 5 mL/kg.
bFormulation, 1.0 mg/mL of 23 in 30% captisol (solution) with dose volume 10 mL/kg.
cFormulation, 5.0 mg/mL of 23 in 30% captisol (solution) with dose volume of 10 mL/kg.
dAUC, area under the curve; Cl, clearance; iv, intravenous, MRT, mean residence time; Vdss, volume of distribution at steady state.

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

Animal Model: Cytoxan-treated DBA-2 mice, Klebsiella pneumoniae MB9249 infection model[1]
Dosage: 10 and 50 mg/kg, in combination with 5mg/kg Imipenem (HY-B1369A)
Administration: Subcutaneous injection, three times a day for 1 day
Result: Demonstrated reduction of bacterial burden in both the spleen and kidney to a greater extent while combining with Imipenem (HY-B1369A) relative to Imipenem (HY-B1369A) alone.
Animal Model: C57BL/6 mice[1]
Dosage: Intravenous and subcutaneous injection
Administration: 5, 10 and 50 mg/kg (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic properties.
分子量

332.34

Formula

C13H12N6O3S

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-9 相关分类

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  • 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.

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HY-152105
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