Zoliflodacin-ETX0914-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZoliflodacinCat. No.: HY-17647CAS No.: 1620458-09-4Synonyms: ETX0914; AZD0914分式: CHFNO分量: 487.44作靶点: DNA/RNA Synthesis; Bacterial作通路: Cell Cycle/DNA Damage; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 month

2、s-20C 1 month溶解性数据体外实验 DMSO : 140 mg/mL (287.21 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0515 mL 10.2577 mL 20.5153 mL5 mM 0.4103 mL 2.0515 mL 4.1031 mL10 mM 0.2052 mL 1.0258 mL 2.0515 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Zoliflodacin (

3、ETX0914;AZD0914)种新型的螺旋嘧啶三酮，细菌DNA促旋酶/拓扑异构酶 抑制剂。Zoliflodacin 对兰阳性和 性物具有有效的体外抗 活性，对 葡萄球菌的bMIC90 值为0.25 g/mL。IC50 & Target MIC90: 0.25 g/mL (S. aureus) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Zoliflodacin has antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphyl

4、ococcusepidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidiousGram-negative (Haemophilus influenzae, Neisseria gonorrhoeae), atypical (Legionella pneumophila), andanaerobic (Clostridium difficile) bacterial species, including isolates with known resis

5、tance tofluoroquinolones. The antibacterial activity of Zoliflodacin is shown to be via inhibition of DNA biosynthesisand accumulation of double-strand cleavages; this mechanism of action differs from those of other marketedantibacterial compounds, including fluoroquinolones. Zoliflodacin stabilizes

6、 and arrests the cleaved covalentcomplex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation ofthe double-strand cleaved DNA to form fused circular DNA 1.PROTOCOLCell Assay 1 Zoliflodacin broth macrodilution MICs are determined and used as the starting poin

7、t for both in vitro time-killand postantibiotic-effect (PAE) tests. In vitro static time-kill studies are conducted with glass tubes (18 by 150mm, without agitation) containing 10-mL volumes of cation-adjusted Mueller-Hinton broth with logarithmicallygrowing cultures (starting inoculum of 1106 CFU/m

8、L) against levofloxacin-susceptible and levofloxacin-resistant S. aureus. Zoliflodacin is tested at concentrations equivalent to 0.5, 1, 2, 4, and 8 times the MIC;samples are plated for colony counts at 0, 2, 4, 6, 8, and 24 h by using 100 L aliquots spotted onto 25-mlsheep blood agar plates as desc

9、ribed previously. Compounds are considered bactericidal at the lowest drugconcentration that reduced viable organism counts by 3 log10 in 24 h. Time-kill studies are conducted induplicate; tests are combined, and mean values are reported 1.MCE has not independently confirmed the accuracy of these me

10、thods. They are for reference only.REFERENCES1. Huband MD, et al. In vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potentactivity against Gram-positive, fastidious Gram-Negative, and atypical bacteria. Antimicrob Agents Chemother. 2015 Jan;59(1):467-74.McePdfHeightCaution: Product has not been fully val