GSK2140944 Gepotidacin
- 公司名稱 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型號 GSK2140944
- 產地
- 廠商性質 生產廠家
- 更新時間 2019/6/27 11:24:57
- 訪問次數 604
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抑制劑，調節劑，API，天然產物，各種類型化合物庫
| 供貨周期 | 現貨 | 規格 | 10 mM * 1 mL；1 mg；5 mg |
|---|---|---|---|
| 貨號 | HY-16742 | 應用領域 | 生物產業 |
Gepotidacin
產品活性：Gepotidacin (GSK2140944)是一種新型的三氮雜苊烯細菌II型拓撲異構酶抑制劑。
研究領域：Anti-infection
作用靶點：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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