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

Enmetazobactam  (Synonyms: AAI101)

製品番号: HY-103095 純度: ≥95.0%
COA 取扱説明書

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

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Enmetazobactam 構造式

Enmetazobactam 構造式

CAS 番号 : 1001404-83-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
1 mg USD 42 在庫あり
5 mg USD 90 在庫あり
10 mg USD 150 在庫あり
50 mg USD 450 在庫あり
100 mg USD 650 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 4 publication(s) in Google Scholar

Other Forms of Enmetazobactam:

Enmetazobactam 関連抗体

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製品説明

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens[1][2].

体外実験

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].

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

Enmetazobactam 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

314.32

分子式

C11H14N4O5S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C[N+]1=NN(C[C@@](S([C@]2([H])C3)(=O)=O)(C)[C@H](C([O-])=O)N2C3=O)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

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

DMSO : ≥ 113.3 mg/mL (360.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: ≥95.0%

COA (253 KB) HNMR (257 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[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.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1815 mL 15.9074 mL 31.8147 mL 79.5368 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL 15.9074 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL 7.9537 mL
15 mM 0.2121 mL 1.0605 mL 2.1210 mL 5.3025 mL
20 mM 0.1591 mL 0.7954 mL 1.5907 mL 3.9768 mL
25 mM 0.1273 mL 0.6363 mL 1.2726 mL 3.1815 mL
30 mM 0.1060 mL 0.5302 mL 1.0605 mL 2.6512 mL
40 mM 0.0795 mL 0.3977 mL 0.7954 mL 1.9884 mL
50 mM 0.0636 mL 0.3181 mL 0.6363 mL 1.5907 mL
60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3256 mL
80 mM 0.0398 mL 0.1988 mL 0.3977 mL 0.9942 mL
100 mM 0.0318 mL 0.1591 mL 0.3181 mL 0.7954 mL
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Enmetazobactam Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Enmetazobactam1001404-83-6AAI101AAI 101AAI-101Beta-lactamaseBacterialβ-lactamaseGram-negativeInhibitorinhibitorinhibit

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