1. Anti-infection
  2. Bacterial
  3. Enmetazobactam

Enmetazobactam (Synonyms: AAI101)

目录号: HY-103095 纯度: 95.11%
产品使用指南

Enmetazobactam (AAI101) 是一种广谱的 β-lactamase 抑制剂,能够抵抗很多耐药革兰氏阴性细菌。

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Enmetazobactam Chemical Structure

Enmetazobactam Chemical Structure

CAS No. : 1001404-83-6

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10 mM * 1 mL in DMSO ¥990
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5 mg ¥900
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10 mg ¥1500
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50 mg ¥4500
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100 mg ¥6500
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.

体外研究
(In Vitro)

Enmetazobactam shows potent activity against specific resistance phenotypes with MIC50 and MIC90 of 0.125 mg/L and 64 mg/L[1]. Cefepime-Enmetazobactam MICs decreases with increasing concentrations of Enmetazobactam (over the range from 1 to 16 mg/L) for most strains, demonstrating a concentration dependence of Enmetazobactam on restoration of the antibacterial activity of the cephalosporin[1].

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

体内研究
(In Vivo)

In neutropenic animals, cefepime-Enmetazobactam treatment results in reductions in bacterial density of ≥0.5 log10 CFU for 12 of the 20 strains tested and reductions of ≥1 log10 CFU for 6 of these. Increases in bacterial density are for only four strains, three of which have cefepime-Enmetazobactam MICs of ≥64 mg/L, irrespective of the Enmetazobactam concentration[2].

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

Clinical Trial
分子量

314.32

Formula

C11H14N4O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : ≥ 113.3 mg/mL (360.46 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1815 mL 15.9074 mL 31.8147 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.62 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[2]

The 20 Enterobacteriaceae strains are used to infect groups of three mice each. At 2 h after inoculation, mice are treated with humanized regimens of cefepime or cefepime-AAI101. All doses are administered as 0.2-mL subcutaneous injections. To serve as control animals, an additional group of mice is administered normal saline at the same volume and frequency and by the same route. Thighs from all animals are harvested at 24 h after initiation of therapy. The harvesting procedure for all study mice began with euthanasia by CO2 exposure, followed by cervical dislocation. After sacrifice, thighs are removed and homogenized individually in normal saline. For determinations of the numbers of CFU, serial dilutions of thigh homogenates are spread onto Trypticase soy agar with 5% sheep blood using a spiral plater. In addition to the aforementioned treatment and control groups, another group of three infected but untreated mice is harvested at the initiation of dosing and served as a 0-h control. Efficacy, expressed as the change in bacterial density, is determined by calculation of the change in the log10 number of CFU obtained in mice after 24 h of treatment from the densities observed in the 0-h control animals.

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

参考文献

纯度: 95.11%

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产品名称:
Enmetazobactam
目录号:
HY-103095
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