GSK2140944 Gepotidacin

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公司名稱 MedChemExpress LLC
品牌 MedChemExpress (MCE)
型號 GSK2140944
產(chǎn)地
廠商性質(zhì) 生產(chǎn)廠家
更新時間 2019/6/27 11:24:57
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GSK2140944 gepotidacin

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詳細(xì)信息 在線詢價

供貨周期	現(xiàn)貨	規(guī)格	10 mM * 1 mL；1 mg,；5 mg
貨號	HY-16742	應(yīng)用領(lǐng)域	生物產(chǎn)業(yè)

Gepotidacin

產(chǎn)品活性：Gepotidacin (GSK2140944)是一種新型的三氮雜苊烯細(xì)菌II型拓?fù)洚悩?gòu)酶抑制劑,。

研究領(lǐng)域：Anti-infection

作用靶點(diǎn)：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.