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Zidebactam

(Synonyms: WCK-5107) Copy Product Info
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Synonyms: WCK-5107

Catalog No. T13395L Copy Product Info
Purity: 99.69%
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Zidebactam (WCK-5107) is a β-lactamase inhibitor and a penicillin-binding protein 2 (PBP2) inhibitor (IC50 = 0.26 μg/ml), with enzymatic inhibitory activity, and can be used for antibacterial research.
Zidebactam
Cas No. 1436861-97-0
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$88In StockIn Stock
5 mg$189In StockIn Stock
10 mg$313In StockIn Stock
25 mg$533In StockIn Stock
50 mg$768In StockIn Stock
100 mg$1,080In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.69%
Color:White
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Product Introduction

Bioactivity
Description
Zidebactam (WCK-5107) is a β-lactamase inhibitor and a penicillin-binding protein 2 (PBP2) inhibitor (IC50 = 0.26 μg/ml), with enzymatic inhibitory activity, and can be used for antibacterial research.
Targets & IC50
Enterobacter spp:0.12 mg/L (MIC50), PBP2:0.26 μg/ml (P. aeruginosa PAO1 PBP2), E. coli:0.12 mg/L (MIC50), Enterobacteriaceae (WT):0.25 mg/L (MIC50)
In vitro
Methods:Acinetobacter baumannii ATCC 19606 and OXA-23-producing clinical ST2 isolates were used to evaluate Zidebactam in vitro activity through MIC determination, PBP binding affinity determination (IC₅₀), and time-kill kinetics assays.
Results: Zidebactam monotherapy showed MIC >1024 μg/mL, but exhibited high affinity for PBP2 (IC₅₀ 0.01 μg/mL); when combined with 8 μg/mL cefepime or sulbactam, MIC decreased by 4-8 fold, with complete bacterial clearance achieved within 24 hours.[1]
Methods: Ninety-three carbapenemase-producing Klebsiella species and other isolates were used to determine the minimum inhibitory concentration (MIC) of Zidebactam alone and in combination with cefepime or ertapenem (1:1) by BSAC agar dilution method, with inoculum ranging from 3-6×10³ to 3-6×10⁵ CFU/spot.
Results: For metallo-β-lactamase-producing strains, the MIC of Zidebactam combinations increased significantly (≥32-fold) with increasing inoculum, while the effect on non-MBL-producing strains was minimal.[2]
In vivo
Methods: A neutropenic mouse pneumonia model was established by intranasal inoculation with Pseudomonas aeruginosa. Zidebactam was administered subcutaneously at doses simulating human alveolar epithelial lining fluid exposure (3.8, 4.15 mg/kg) every 8 hours for 24 hours, with normal saline as the vehicle.
Results: Zidebactam monotherapy reduced bacterial load by 0.99 log₁₀ CFU/lung, while combination with cefepime (WCK 5222) increased the reduction to 2.21 log₁₀ CFU/lung, demonstrating synergistic enhancement.[3]
Methods: A neutropenic mouse pneumonia model was established by intranasal inoculation with Acinetobacter baumannii. Zidebactam was administered subcutaneously at doses of 12.5 and 37.5 mg/kg every 2 hours for 24 hours, with normal saline as the vehicle.
Results: Zidebactam monotherapy was ineffective, but when combined with cefepime, it reduced the percentage of time that free drug concentrations exceeded the MIC required for 1-log₁₀ bactericidal activity from 38.9% to 15.5%.[4]
SynonymsWCK-5107
Chemical Properties
Molecular Weight391.4
FormulaC13H21N5O7S
Cas No.1436861-97-0
SmilesOS(=O)(=O)ON1[C@H]2CN([C@@H](CC2)C(=O)NNC(=O)[C@@H]2CCCNC2)C1=O
Relative Density.no data available
Storage & Solubility Information
StorageStore at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (638.73 mM), Sonication is recommended.
H2O: 50 mg/mL (127.75 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.77 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.5549 mL12.7747 mL25.5493 mL127.7466 mL
5 mM0.5110 mL2.5549 mL5.1099 mL25.5493 mL
10 mM0.2555 mL1.2775 mL2.5549 mL12.7747 mL
20 mM0.1277 mL0.6387 mL1.2775 mL6.3873 mL
50 mM0.0511 mL0.2555 mL0.5110 mL2.5549 mL
100 mM0.0255 mL0.1277 mL0.2555 mL1.2775 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Keywords

Related Tags: Zidebactam chemical structure | Zidebactam in vivo | Zidebactam in vitro | Zidebactam formula | Zidebactam molecular weight