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

Zoliflodacin (Synonyms: ETX0914; AZD0914)

Cat. No.: HY-17647 Purity: >98.0%
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
10 mM * 1 mL in DMSO USD 429 In-stock
Estimated Time of Arrival: December 31
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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

MIC90: 0.25 μg/mL (S. aureus)[1]

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 140 mg/mL (287.21 mM; Need ultrasonic)

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
10 mM 0.2052 mL 1.0258 mL 2.0515 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

487.44

Formula

C₂₂H₂₂FN₅O₇

CAS No.

1620458-09-4

SMILES

O=C(NC(C12[[email protected]]([[email protected]](C)O[[email protected]](C)C3)([H])N3C4=C(C=C5C(ON=C5N6C(OC[[email protected]@H]6C)=O)=C4F)C2)=O)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Zoliflodacin
Cat. No.:
HY-17647
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Zoliflodacin

Cat. No.: HY-17647