Zoliflodacin
Based on 6 publication(s) in Google Scholar
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 μg/mL.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1620458-09-4
- Formula: C22H22FN5O7
- Molecular Weight:487.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Zoliflodacin
More- Sci Rep. 2024 Jan 12;14(1):1179. [Abstract]
- ACS Infect Dis. 2026 Feb 13;12(2):816-826. [Abstract]
- ACS Infect Dis. 2024 Oct 11;10(10):3631-3639. [Abstract]
- ACS Infect Dis. 2024 Aug 9;10(8):3071-3082. [Abstract]
- ACS Infect Dis. 2023 Mar 10;9(3):706-715. [Abstract]
- Int J STD AIDS. 2024 Sep 3:9564624241280082. [Abstract]
All DNA/RNA Synthesis Isoforms
MoreAll Antibiotic Isoforms
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Biological Activity
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Quinolone |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>50 μM
Compound: Zoliflodacin
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
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[PMID: 35500229] |
Zoliflodacin has antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae, Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. The antibacterial activity of Zoliflodacin is shown to be via inhibition of DNA biosynthesis and accumulation of double-strand cleavages; this mechanism of action differs from those of other marketed antibacterial compounds, including fluoroquinolones. Zoliflodacin stabilizes and arrests the cleaved covalent complex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation of the double-strand cleaved DNA to form fused circular DNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1620458-09-4
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Appearance Solid
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Molecular Weight 487.44
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Formula C22H22FN5O7
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Color White to off-white
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SMILES
O=C(NC(C12[C@]([C@H](C)O[C@H](C)C3)([H])N3C4=C(C=C5C(ON=C5N6C(OC[C@@H]6C)=O)=C4F)C2)=O)NC1=O
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Synonyms
ETX0914; AZD0914
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Rep
Gonococcal resistance to zoliflodacin could emerge via transformation from commensal Neisseria species. An in-vitro transformation study. [Abstract]2024 Jan 12;14(1):1179. PMID: 38216602 -
ACS Infect Dis
Enzyme-DNA Interactions Affect the Catalytic Inhibition of Mycobacterial Gyrases by Antibacterial Drugs. [Abstract]2026 Feb 13;12(2):816-826. PMID: 41591340 -
ACS Infect Dis
Role of DNA Double-Strand Break Formation in Gyrase Inhibitor-Mediated Killing of Nonreplicating Persistent Mycobacterium tuberculosis in Caseum. [Abstract]2024 Oct 11;10(10):3631-3639. PMID: 39315541 -
ACS Infect Dis
Interactions between Zoliflodacin and Neisseria gonorrhoeae Gyrase and Topoisomerase IV: Enzymological Basis for Cellular Targeting. [Abstract]2024 Aug 9;10(8):3071-3082. PMID: 39082980 -
ACS Infect Dis
A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated by Mycobacterium tuberculosis Gyrase. [Abstract]2023 Mar 10;9(3):706-715. PMID: 36802491 -
Int J STD AIDS
Assessing novel partner antimicrobials to protect ceftriaxone against gonococcal resistance: An in vitro evaluation. [Abstract]2024 Sep 3:9564624241280082. PMID: 39226039
Solvent & Solubility
DMSO : 140 mg/mL (287.21 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.27 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 (4.27 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.
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.
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.
Protocol
Zoliflodacin broth macrodilution MICs are determined and used as the starting point for both in vitro time-kill and postantibiotic-effect (PAE) tests. In vitro static time-kill studies are conducted with glass tubes (18 by 150 mm, without agitation) containing 10-mL volumes of cation-adjusted Mueller-Hinton broth with logarithmically growing cultures (starting inoculum of 1×106 CFU/mL) against levofloxacin-susceptible and levofloxacin-resistant S. aureus. Zoliflodacin is tested at concentrations equivalent to 0.5, 1, 2, 4, and 8 times the MIC; samples are plated for colony counts at 0, 2, 4, 6, 8, and 24 h by using 100 μL aliquots spotted onto 25-ml sheep blood agar plates as described previously. Compounds are considered bactericidal at the lowest drug concentration that reduced viable organism counts by ≥3 log10 in 24 h. Time-kill studies are conducted in duplicate; tests are combined, and mean values are reported[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (294 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0515 mL | 10.2577 mL | 20.5153 mL | 51.2884 mL |
| 5 mM | 0.4103 mL | 2.0515 mL | 4.1031 mL | 10.2577 mL | |
| 10 mM | 0.2052 mL | 1.0258 mL | 2.0515 mL | 5.1288 mL | |
| 15 mM | 0.1368 mL | 0.6838 mL | 1.3677 mL | 3.4192 mL | |
| 20 mM | 0.1026 mL | 0.5129 mL | 1.0258 mL | 2.5644 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8206 mL | 2.0515 mL | |
| 30 mM | 0.0684 mL | 0.3419 mL | 0.6838 mL | 1.7096 mL | |
| 40 mM | 0.0513 mL | 0.2564 mL | 0.5129 mL | 1.2822 mL | |
| 50 mM | 0.0410 mL | 0.2052 mL | 0.4103 mL | 1.0258 mL | |
| 60 mM | 0.0342 mL | 0.1710 mL | 0.3419 mL | 0.8548 mL | |
| 80 mM | 0.0256 mL | 0.1282 mL | 0.2564 mL | 0.6411 mL | |
| 100 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5129 mL |
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