2. Anti-infection
  3. Bacterial Beta-lactamase
  4. Pilabactam

Pilabactam (ANT3310) 是一种广谱的、共价的丝氨酸 β-内酰胺酶 (Serine β-Lactamase) 抑制剂，IC50 值为 1 nM-175 nM (一系列丝氨酸β-内酰胺酶)。Pilabactam 增强 β-内酰胺类抗生素对耐碳青霉烯类肠杆菌 (CRE) 和鲍曼不动杆菌 (CRAB) 的活性。Pilabactam 可用于细菌感染相关的研究。

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Pilabactam

Pilabactam Chemical Structure

CAS No. : 2410688-60-5

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Pilabactam 的其他形式现货产品:

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Pilabactam 相关抗体

Top Publications Citing Use of Products

查看 Beta-lactamase 亚型特异性产品:

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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

Pilabactam (ANT3310) is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam can be used in the research of bacterial infection[1][2].

体外研究
(In Vitro)

Pilabactam (Compound 21，0.006-3 000 nM，10 分钟) 可抑制一系列丝氨酸 β-内酰胺酶 (AmpC、CTX-M-15、TEM-1、OXA-48、OXA-23 和 KPC-2)，IC50 值范围为 1 nM 至 175 nM[1]。
Pilabactam 在 HepG2 细胞中表现出较低的 in vitro 细胞毒性 (IC50: > 100 μM)，心脏毒性 (抑制 hERG 钾离子通道) 和遗传毒性 (Ames 试验) [1]。

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

Pilabactam 相关抗体:
体内研究
(In Vivo)

Pilabactam (静脉注射，25-100 mg/kg，感染后 1、3、5 和 7 小时) 可降低小鼠大腿感染模型中的细菌负担[1]。
Pilabactam (静脉注射，1 mg/kg，雄性瑞士白化小鼠) 的 T1/2 值为 0.64 h，AUC 值为 412 ng•h/mL，Cl 值为 40 mL/min/kg (药代动力学测定)[1]。

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

Animal Model: Murine thigh infection model[1]
Dosage: 25, 50, and 100 mg/kg
Administration: Intravenous injection, at 1, 3, 5, and 7 h postinfection
Result: Reduced bacterial burdens (colony forming units, CFU) in a dose-dependent manner to levels below that of the initial starting inoculum at the highest dose, when treated with the combination of MEM.
分子量

240.21

Formula

C6H9FN2O5S
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

Pilabactam 相关分类

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  • 稀释计算器

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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.

Keywords:

Pilabactam2410688-60-5ANT3310ANT 3310ANT-3310BacterialBeta-lactamaseβ-lactamaseDBOsSBLCRECRABOXA enzymesβ-lactam antibioticinfectionInhibitorinhibitorinhibit

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