| Size | Price | Stock | Qty |
|---|---|---|---|
| 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 |
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Zidebactam (WCK-5107; WCK5107) is a potent β-lactamase inhibitor and also a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL. It is one of the components ot WCK 5222 (Cefepime-Zidebactam) which is a bicyclo-acyl hydrazide β-lactam enhancer antibiotic with a dual action involving binding to Gram-negative bacterial PBP2 and β-lactamase inhibition. Cefepime/zidebactam demonstrated excellent activity against Enterobacteriaceae and P. aeruginosa, although activity was reduced in carbapenem-non-susceptible isolates. The activity against A. baumannii was reduced and studies examining the therapeutic efficacy in strains with high cefepime/zidebactam MICs are warranted.
| 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].
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| References |
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| Additional Infomation |
Zidebactam is under investigation in clinical trial NCT02674347 (MAD Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Intravenous Zidebactam in Healthy Adults).
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| 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
|
| 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) |
|---|---|
| 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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