2. Anti-infection
  3. Bacterial Beta-lactamase
  4. MBL-IN-5

MBL-IN-5 是一种金属-β-内酰胺酶 (MBL) 抑制剂。MBL-IN-5 可抑制三种临床相关的 B1 亚家族 MBL (NDM-1、 VIM-1 和 IMP-1)，IC50 分别为 0.05 nM、 14 nM 和 21 nM。MBL-IN-5 显著增强 carbapenems 抗生素对产 MBL 临床菌株的疗效，且与 IPM 抗生素联合使用可显著降低大腿感染模型中的细菌负荷。

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MBL-IN-5 Chemical Structure

MBL-IN-5 Chemical Structure

CAS No. : 2876921-34-3

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MBL-IN-5 相关抗体

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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

MBL-IN-5 is a metallo-β-lactamase (MBL) inhibitor. MBL-IN-5 inhibits three clinically relevant B1 subfamily MBLs (NDM-1, VIM-1, and IMP-1) with IC50s of 0.05  nM, 14  nM and 21 nM respectively. MBL-IN-5 remarkably enhances carbapenems’ effectiveness against MBL-producing clinical strains and significantly reduces the bacterial load in a neutropenic murine thigh infection model combined with the IPM antibiotic[1].

IC50 & Target[1]

NDM-1

0.05 nM (IC50)

IMP-1

21 nM (IC50)

VIM-1

14 nM (IC50)

体外研究
(In Vitro)

MBL-IN-5 (Compound 17u) (4-32 μg/mL，16-18 小时) 与 Imipenem (IPM) (HY-B1369A) 和 Meropenem (HY-13678) 表现出强大的协同作用，可对抗表达新德里金属-β-内酰胺酶-1 (NDM-1) 的耐 carbapenem 的 Klebsiella pneumoniae ATCC BAA-2146[1]。
MBL-IN-5 (3.12-50 μM) 可强效稳定 NDM-1，使 Tm 正向偏移约 ~15-20 °C[1]。
MBL-IN-5 (1-500 μM) 具有理想的 ADME 特性，表现出中等溶解度、高渗透性和中等清除率[1]。
MBL-IN-5 (0.5-16 μg/mL，16-18 小时) 可有效抑制 NDM-1，使所有受试 ATCC 菌株恢复对 Meropenem 和 IPM 的敏感性 (MIC 降低数倍)，并且与 Meropenem 或 IPM 联合使用时可高度抑制表达 NDM-1 的肠杆菌科临床菌株[1]。
MBL-IN-5 对 MBL 的特异性高于对 MMP 的特异性，其对 MMP-1、 MMP-2 和 MMP-9 的 IC50 分别为 >120 μM、2.9 μM 和 45 μM[1]。

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

MBL-IN-5 相关抗体:
体内研究
(In Vivo)

MBL-IN-5 (Compound 17u) (20-50 mg/kg，皮下注射，每8小时1次，共3次) 与 IPM 联合使用时，可显著提高中性粒细胞减少性小鼠大腿感染模型中 IPM 对表达 NDM-1、耐 carbapenem 的 Klebsiella pneumonia ATCC BAA 2146 的活性，并降低细菌负荷[1]。

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

Animal Model: female BALB/c mice (6-8 weeks old) were given two intraperitoneal cyclophosphamide injections 4 days and 1 day and then injected into the left thighs with 0.05 mL diluted culture of NDM-1 expressing Klebsiella pneumonia ATCC BAA 2146 (5 × 105 CFU/ mouse)[1].
Dosage: alone: 50 mg/kg, combination: 10 mg/kg IPM + 20 mg/kg MBL-IN-5
Administration: s.c., following 2 h postinfection, every 8 h for 3 times and then collects thighs to compare the CFU at 26 h.
Result: Enhanced the activity of IPM against carbapenem-resistant NDM-1-expressing Klebsiella pneumonia ATCC BAA 2146 and significantly reduced ~2.2 log10 CFU/mL/thigh combined with IPM.
分子量

353.80

Formula

C20H16ClNO3
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

MBL-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MBL-IN-52876921-34-3BacterialBeta-lactamaseβ-lactamaseInhibitorsAntimicrobialNeutropenic murine thigh infection modelImipenem (IPM)Inhibitorinhibitorinhibit

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