1. Cell Cycle/DNA Damage Anti-infection
  2. DNA/RNA Synthesis Bacterial Antibiotic
  3. Zoliflodacin

Zoliflodacin  (Synonyms: ETX0914; AZD0914)

Cat. No.: HY-17647 Purity: 99.95%
COA Handling Instructions

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.

Zoliflodacin Chemical Structure

Zoliflodacin Chemical Structure

CAS No. : 1620458-09-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 354 In-stock
Solution
10 mM * 1 mL in DMSO USD 354 In-stock
Solid
5 mg USD 330 In-stock
10 mg USD 520 In-stock
25 mg USD 990 In-stock
50 mg USD 1600 In-stock
100 mg USD 2600 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

Quinolone

 

In Vitro

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.

Clinical Trial
Molecular Weight

487.44

Formula

C22H22FN5O7

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0515 mL 10.2577 mL 20.5153 mL
5 mM 0.4103 mL 2.0515 mL 4.1031 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.95%

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Zoliflodacin
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