Gepotidacin

SKU: orb1709615

Description

Gepotidacin is a structurally novel triazaacenaphthylene antibacterial agent targeting bacterial type II topoisomerases. It shows potent in vitro and in vivo activity against resistant pathogens, including multidrug-resistant Neisseria gonorrhoeae and Staphylococcus aureus, making it a promising candidate for antibacterial research.

Research Area

Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 1075236-89-3
• MW: 448.52
• Formula: C₂₄H₂₈N₆O₃
• SMILES: O=c1ccc2ncc(=O)n3[C@H](CN4CCC(CC4)NCc4cc5CCCOc5cn4)Cn1c23
• Target: Others
• Solubility: DMSO:5.5 mg/mL (12.26 mM)

Bioactivity

• In Vivo:
  For six methicillin-resistant Staphylococcus vitis vinifera (MRSA) isolates, the minimum inhibitory concentration (MIC) of Gepotidacin ranged between 0.125~0.5 mg/L. The alveolar epithelial lining fluid (ELF) penetration ratio of this drug was 1.1~1.4. In a neutropenic murine model, the maximum bacterial clearance effect reached 1.1~3.1 log10 CFU. The mean free drug area under the curve to minimum inhibitory concentration ratios (fAUC/MIC) required to achieve bacterial growth stasis and a 1-log reduction were 59.3 ± 34.6 and 148.4 ± 83.3, respectively .
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• In Vitro:
  Gepotidacin has in vitro activity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs) . Gepotidacin inhibits bacterial DNA gyrase and topoisomerase IV via a unique mechanism and has demonstrated in vitro activity against gram-negative and gram-positive bacteria, including drug-resistant strains. It also targets pathogens associated with other conventional and biothreat infections. The MIC50 and MIC90 for gepotidacin against the 25 N. gonorrhoeae isolates tested are 0.12 and 0.25 μg/mL, respectively . The gepotidacin MIC90s are as follows: Streptococcus pyogenes (0.25 μg/mL), Escherichia coli (2 μg/mL), Moraxella catarrhalis (≤0.06 μg/mL), Streptococcus pneumoniae (0.25 μg/mL), Haemophilus influenzae (1 μg/mL), Clostridium perfringens (0.5 μg/mL), and Shigella spp. (1 μg/mL) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK2140944, GSK 2140944, GSK-2140944, Gepotidacin

Compound Identifiers

PubChem CID

25101874