Zoliflodacin
(Synonyms: ETX0914; AZD0914) 目录号 : GC19391A fluoroquinolone antibiotic
Cas No.:1620458-09-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: |
Zoliflodacin broth macrodilution MICs are determined and used as the starting point for both in vitro time-kill and postantibiotic-effect (PAE) tests. In vitro static time-kill studies are conducted with glass tubes (18 by 150 mm, without agitation) containing 10-mL volumes of cation-adjusted Mueller-Hinton broth with logarithmically growing cultures (starting inoculum of 1×106 CFU/mL) 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 μL aliquots spotted onto 25-ml sheep blood agar plates as described previously. Compounds are considered bactericidal at the lowest drug concentration that reduced viable organism counts by ≥3 log10 in 24 h. Time-kill studies are conducted in duplicate; tests are combined, and mean values are reported[1]. |
References: [1]. Huband MD, et al. In vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potent activity against Gram-positive, fastidious Gram-Negative, and atypical bacteria. Antimicrob Agents Chemother. 2015 Jan;59(1):467-74. |
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 ug/mL.
Zoliflodacin has antibacterial activity against key Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae, Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial species, including isolates with known resistance to fluoroquinolones. The antibacterial activity of Zoliflodacin is shown to be via inhibition of DNA biosynthesis and accumulation of double-strand cleavages; this mechanism of action differs from those of other marketed antibacterial compounds, including fluoroquinolones. Zoliflodacin stabilizes and arrests the cleaved covalent complex of gyrase with double-strand broken DNA under permissive conditions and thus blocks religation of the double-strand cleaved DNA to form fused circular DNA[1].
References:
[1]. Huband MD, et al. In vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potent activity against Gram-positive, fastidious Gram-Negative, and atypical bacteria. Antimicrob Agents Chemother. 2015 Jan;59(1):467-74.
Cas No. | 1620458-09-4 | SDF | |
别名 | ETX0914; AZD0914 | ||
Canonical SMILES | O=C(NC(C12[C@]([C@H](C)O[C@H](C)C3)([H])N3C4=C(C=C5C(ON=C5N6C(OC[C@@H]6C)=O)=C4F)C2)=O)NC1=O | ||
分子式 | C22H22FN5O7 | 分子量 | 487.44 |
溶解度 | DMSO : 140 mg/mL (287.21 mM) | 储存条件 | Store at -20°C |
General tips | 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0515 mL | 10.2577 mL | 20.5153 mL |
5 mM | 0.4103 mL | 2.0515 mL | 4.1031 mL |
10 mM | 0.2052 mL | 1.0258 mL | 2.0515 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。