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。

Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

Solid

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 has in vitro activity against causative pathog

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3).
[2]. Biedenbach DJ, et al. In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens. Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23.

In Vitro: DMSO : 7.14 mg/mL (15.92 mM; Need ultrasonic)配制储备液