Enmetazobactam
Based on 6 publication(s) in Google Scholar
Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
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- Pureza: 98.69%
- No. CAS: 1001404-83-6
- Fòrmula: C11H14N4O5S
- Peso molecular:314.32
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Enmetazobactam
More- Int J Antimicrob Agents. 2023 Apr;61(4):106738. [Abstract]
- ACS Infect Dis. 2021 Apr 9;7(4):826-837. [Abstract]
- Antimicrob Agents Chemother. 2026 Jun 3;70(6):e0126725. [Abstract]
- Antimicrob Agents Chemother. 2024 Nov 6;68(11):e0077524. [Abstract]
- Antimicrob Agents Chemother. 2023 Jul 18;67(7):e0033923. [Abstract]
- Antimicrob Agents Chemother. 2022 Feb 15;66(2):e0167621. [Abstract]
Ver todos los productos específicos de isoformas Beta-lactamase
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Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1001404-83-6
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Appearance Solid
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Peso molecular 314.32
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Fòrmula C11H14N4O5S
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Color White to off-white
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SMILES
C[N+]1=NN(C[C@@](S([C@]2([H])C3)(=O)=O)(C)[C@H](C([O-])=O)N2C3=O)C=C1
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Synonyms
AAI101
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Int J Antimicrob Agents
Activity of aztreonam in combination with novel β-lactamase inhibitors against metallo-β-lactamase-producing Enterobacterales from Spain. [Abstract]2023 Apr;61(4):106738. PMID: 36736925 -
ACS Infect Dis
Assessing the Potency of β-Lactamase Inhibitors with Diverse Inactivation Mechanisms against the PenA1 Carbapenemase from Burkholderia multivorans. [Abstract]2021 Apr 9;7(4):826-837. PMID: 33723985 -
Antimicrob Agents Chemother
Improved hydrolysis of piperacillin by OXA-48-like R214G variants, a selective advantage under piperacillin-tazobactam exposure. [Abstract]2026 Jun 3;70(6):e0126725. PMID: 42053451 -
Antimicrob Agents Chemother
Relative inhibitory activities of newly developed diazabicyclooctanes, boronic acid derivatives, and penicillin-based sulfone β-lactamase inhibitors against broad-spectrum AmpC β-lactamases. [Abstract]2024 Nov 6;68(11):e0077524. PMID: 39365068 -
Antimicrob Agents Chemother
Impact of Acquired Broad Spectrum β-Lactamases on Susceptibility to Novel Combinations Made of β-Lactams (Aztreonam, Cefepime, Meropenem, and Imipenem) and Novel β-Lactamase Inhibitors in Escherichia coli and Pseudomonas aeruginosa. [Abstract]2023 Jul 18;67(7):e0033923. PMID: 37255469 -
Antimicrob Agents Chemother
Assessment of Activity and Resistance Mechanisms to Cefepime in Combination with the Novel β-Lactamase Inhibitors Zidebactam, Taniborbactam, and Enmetazobactam against a Multicenter Collection of Carbapenemase-Producing Enterobacterales. [Abstract]2022 Feb 15;66(2):e0167621. PMID: 34807754
Solvente y solubilidad
DMSO : ≥ 113.3 mg/mL (360.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (318.15 mM)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Crandon JL, et al. In Vitro Activity of Cefepime/AAI101 and Comparators against Cefepime Non-susceptible Enterobacteriaceae. Pathogens. 2015 Aug 18;4(3):620-5. [Content Brief]
[2]. Crandon JL, et al. In vivo activities of simulated human doses of cefepime and cefepime-AAI101 against multidrug-resistant Gram-negative Enterobacteriaceae. Antimicrob Agents Chemother. 2015 May;59(5):2688-94. [Content Brief]
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 |
|---|---|---|---|---|---|
| H2O / 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 |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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