GSK2140944-Gepotidacin_抗感染-MedChemExpress LLC

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产品简介 品牌 MedChemExpress (MCE) 货号 HY-16742 规格 10 mM * 1 mL；1 mg；5 mg 供货周期 现货 应用领域 生物产业     Gepotidacin （GSK2140944）是一种新型的三氮杂苊烯细菌II型拓扑异构酶抑制剂。
详细介绍 Gepotidacin

产品活性：Gepotidacin (GSK2140944)是一种新型的三氮杂苊烯细菌II型拓扑异构酶抑制剂。

研究领域：Anti-infection

作用靶点：Bacterial

In Vitro: Gepotidacin is a novel, first-in-class, triazaacenaphthylene antibacterial that inhibits bacterial DNA gyrase and topoisomerase IV via a unique mechanism and has demonstrated in vitro activity against gram-negative and gram-positive bacterias , including drug-resistant strains, and 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 (in μg/mL): Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤0.06; Streptococcus pneumoniae, 0.25; Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1. Gepotidacin hasin vitroactivity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs).

In Vivo: GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. ELF penetration ratios range from 1.1 to 1.4. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 34.6 and 148.4 83.3, respectively.

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