| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Zidebactam targets penicillin-binding protein 2 (PBP2) in Gram-negative bacteria with high affinity. It also inhibits a broad range of β-lactamases, including class A, C, and D enzymes. By inhibiting both PBP2 and β-lactamases, Zidebactam possesses intrinsic antibacterial activity and enhances the efficacy of existing antibiotics against resistant bacterial strains.
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| ln Vitro |
Zidebactam (WCK-5107) has a MIC50 of 0.25 mg/L and inhibits WT Enterobacteriaceae. When tested against E. coli (MIC50/90 0.12/0.12 mg/L) and Enterobacter spp. (MIC50/90 0.12/0.25 mg/L), zebebactam alone exhibited varied efficacy [1].
Zidebactam is a potent PBP2 inhibitor with an IC50 of 0.26 μg/mL. It is a potent β-lactamase inhibitor. The compound possesses intrinsic antibacterial activity. Zidebactam enhances the efficacy of existing antibiotics against multidrug-resistant Gram-negative bacterial infections. |
| ln Vivo |
Zidebactam is undergoing clinical development for the treatment of carbapenem-resistant Gram-negative infections. As a potent PBP2 and β-lactamase inhibitor, it is expected to exhibit efficacy in preclinical and clinical models of bacterial infections. Further research is needed to fully characterize its pharmacokinetic and pharmacodynamic profiles.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for Zidebactam typically involves measuring its inhibitory activity against PBP2 and β-lactamases using standard biochemical assays. The compound is incubated with the enzyme and a substrate, and the enzymatic activity is measured. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
The in vitro cellular assay for Zidebactam typically involves culturing bacterial strains in appropriate growth media. Bacteria are treated with varying concentrations of the compound, and bacterial growth is measured using standard assays such as broth microdilution. The minimum inhibitory concentration (MIC) is determined from the dose-response curve. The compound's ability to enhance the efficacy of other antibiotics is also assessed.
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| Animal Protocol |
In vivo animal studies for Zidebactam would typically involve the use of mouse models of bacterial infection. Animals would be infected with carbapenem-resistant Gram-negative bacteria and administered the compound via appropriate routes (e.g., intravenous or subcutaneous injection) at various dose levels. Bacterial load in tissues would be measured, and survival rates would be monitored.
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| ADME/Pharmacokinetics |
Zidebactam has a molecular weight of 391.40 g/mol and a molecular formula of C13H21N5O7S. The IUPAC name is (1R,2S,5R)-7-Oxo-2-(2-((R)-piperidine-3-carbonyl)hydrazine-1-carbonyl)-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate. The compound has a purity of ≥98%. Further detailed physicochemical properties are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for Zidebactam are not extensively reported in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
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| References |
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| Additional Infomation |
Zidebactam is being studied in the clinical trial NCT02674347 (the MAD study, an evaluation of the safety, tolerability, and pharmacokinetics of intravenous zidebactam in healthy adults).
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor that also acts as a penicillin-binding protein 2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL. It is a non-β-lactam antibiotic categorized as a diazabicyclooctane (DBO). The compound is undergoing clinical development for the treatment of carbapenem-resistant Gram-negative infections. It is also known by the synonym WCK-5107. |
| Molecular Formula |
C13H21N5O7S
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|---|---|
| Molecular Weight |
391.4
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| Exact Mass |
391.116
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| Elemental Analysis |
C, 39.89; H, 5.41; N, 17.89; O, 28.61; S, 8.19
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| CAS # |
1436861-97-0
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| Related CAS # |
Zidebactam sodium salt;1706777-46-9
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| PubChem CID |
77846445
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| Appearance |
White to off-white solid powder.
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.653
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| LogP |
-3.01
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
694
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| Defined Atom Stereocenter Count |
3
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| SMILES |
[N@]12C[C@H](N(OS(=O)(O)=O)C1=O)CC[C@H]2C(NNC([C@@H]1CCCNC1)=O)=O
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| InChi Key |
YCZPXRQPDCXTIO-BBBLOLIVSA-N
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| InChi Code |
InChI=1S/C13H21N5O7S/c19-11(8-2-1-5-14-6-8)15-16-12(20)10-4-3-9-7-17(10)13(21)18(9)25-26(22,23)24/h8-10,14H,1-7H2,(H,15,19)(H,16,20)(H,22,23,24)/t8-,9-,10+/m1/s1
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| Chemical Name |
(1R,2S,5R)-7-oxo-2-(2-((R)-piperidine-3-carbonyl)hydrazine-1-carbonyl)-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate
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| Synonyms |
WCK-5107; WCK 5107; WCK5107; Zidebactam
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~638.73 mM)
H2O : ~100 mg/mL (~255.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 1.98 mg/mL (5.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (255.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5549 mL | 12.7747 mL | 25.5493 mL | |
| 5 mM | 0.5110 mL | 2.5549 mL | 5.1099 mL | |
| 10 mM | 0.2555 mL | 1.2775 mL | 2.5549 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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