WCK-4234
Based on 1 Customer Validation
WCK-4234 is a diazabicyclooctane β-lactamase inhibitor and susceptibility restorer. WCK-4234 lacks direct antibacterial activity. WCK-4234 inhibits class A, C, D β-lactamases and extended-spectrum β-lactamases to potentiate Imipenem (HY-B1369A) and Meropenem (HY-13678) activity against Gram-negative pathogens. WCK-4234 can be used for the research of gram-negative bacterial infections and β-lactamase-mediated carbapenem-resistant bacterial infections.
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- Pureté: 98.0%
- CAS No.: 1804915-68-1
- Formule: C7H8N3NaO5S
- Masse moléculaire:269.21
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
WCK-4234 (4-8 mg/L) potently potentiates imipenem and meropenem against clinical Enterobacteriaceae isolates with KPC, OXA-48, or OXA-181 carbapenemases, or combinations of AmpC/ESBL activity and impermeability, reducing geometric mean carbapenem MICs to ≤1 mg/L, but does not potentiate carbapenems against MBL-producing Enterobacteriaceae[2].
WCK-4234 (4-8 mg/L) potentiates imipenem and meropenem against AmpC-hyperproducing, OprD-deficient, and OXA-181-producing Pseudomonas aeruginosa isolates, reducing carbapenem MIC50s by 4-fold or more, but does not potentiate carbapenems against MBL-producing Pseudomonas aeruginosa[2].
WCK-4234 (4-8 mg/L) potently potentiates imipenem and meropenem against OXA-23-producing and hyperproduced OXA-51-producing Acinetobacter baumannii isolates, reducing geometric mean carbapenem MIC50s by 8-40-fold to ≤2 mg/L in most cases, but does not potentiate carbapenems against MBL-producing Acinetobacter baumannii[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1804915-68-1
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Appearance Solid
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Masse moléculaire 269.21
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Formule C7H8N3NaO5S
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Color Off-white to light yellow
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SMILES
O=S(ON1[C@@H]2CC[C@@H](C#N)[N@@](C2)C1=O)(O[Na])=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (371.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (9.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (9.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Iregui A, et al. Activity of Meropenem with a Novel Broader-Spectrum β-Lactamase Inhibitor, WCK 4234, against Gram-Negative Pathogens Endemic to New York City. Antimicrob Agents Chemother. 2019 Dec 20;64(1):e01666-19. [Content Brief]
[2]. Mushtaq S, et al. WCK 4234, a novel diazabicyclooctane potentiating carbapenems against Enterobacteriaceae, Pseudomonas and Acinetobacter with class A, C and D β-lactamases. J Antimicrob Chemother. 2017 Jun 1;72(6):1688-1695. [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 (sealed storage, away from moisture). 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 | 3.7146 mL | 18.5729 mL | 37.1457 mL | 92.8643 mL |
| 5 mM | 0.7429 mL | 3.7146 mL | 7.4291 mL | 18.5729 mL | |
| 10 mM | 0.3715 mL | 1.8573 mL | 3.7146 mL | 9.2864 mL | |
| 15 mM | 0.2476 mL | 1.2382 mL | 2.4764 mL | 6.1910 mL | |
| 20 mM | 0.1857 mL | 0.9286 mL | 1.8573 mL | 4.6432 mL | |
| 25 mM | 0.1486 mL | 0.7429 mL | 1.4858 mL | 3.7146 mL | |
| 30 mM | 0.1238 mL | 0.6191 mL | 1.2382 mL | 3.0955 mL | |
| 40 mM | 0.0929 mL | 0.4643 mL | 0.9286 mL | 2.3216 mL | |
| 50 mM | 0.0743 mL | 0.3715 mL | 0.7429 mL | 1.8573 mL | |
| 60 mM | 0.0619 mL | 0.3095 mL | 0.6191 mL | 1.5477 mL | |
| 80 mM | 0.0464 mL | 0.2322 mL | 0.4643 mL | 1.1608 mL | |
| 100 mM | 0.0371 mL | 0.1857 mL | 0.3715 mL | 0.9286 mL |
- WCK-4234
- 1804915-68-1
- WCK4234
- WCK 4234
- Beta-lactamase
- Bacterial
- Pseudomonas aeruginosa
- extended-spectrum β-lactamases
- Gram-negative pathogens
- carbapenem-resistant bacterial infections
- Enterobacteriaceae
- β-lactamase inhibitor
- Acinetobacter baumannii
- class A β-lactamases
- class D β-lactamases
- class C β-lactamases
- Inhibitor
- inhibitor
- inhibit