Zabofloxacin hydrochloride
(Synonyms: DW-224a) 目录号 : GC37958
Zabofloxacin hydrochloride (DW-224a) 是一种新型氟萘啶酮喹诺酮，被认为是临床试验的有效抗菌候选物。Zabofloxacin hydrochloride (DW-224a) 具有抗革兰氏阳性病原体的优良活性，包括金黄色葡萄球菌 (S. aureus)，化脓性链球菌(S. pyrigenes)和肺炎链球菌(S. pneumonia)。Zabofloxacin hydrochloride (DW-224a) 被认为是治疗喹诺酮类易感和喹诺酮类耐药性淋病的替代药物。
Cas No.:623574-00-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.Zabofloxacin hydrochloride (DW-224a) has excellent activity against gram-positive pathogens including Steptococcus aureus (S. aureus), Streptococcus pyogenes (S. pyrigenes), and S. pneumonia.Zabofloxacin hydrochloride (DW-224a) is considered as an alternative candidate for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP)[1].
[1]. Park HS, et al. Antimicrobial Activity of Zabofloxacin against Clinically Isolated Streptococcus pneumoniae. Molecules. 2016 Nov 17;21(11). pii: E1562.
| Cas No. | 623574-00-5 | SDF | |
| 别名 | DW-224a | ||
| Canonical SMILES | O=C(O)C1=CN(C2=NC(N(CC/34CNC4)CC3=N\OC)=C(C=C2C1=O)F)C5CC5.[H]Cl | ||
| 分子式 | C19H21ClFN5O4 | 分子量 | 437.85 |
| 溶解度 | DMSO : 6.67 mg/mL (15.23 mM; ultrasonic and warming and heat to 60°C) | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2839 mL | 11.4194 mL | 22.8389 mL |
| 5 mM | 0.4568 mL | 2.2839 mL | 4.5678 mL |
| 10 mM | 0.2284 mL | 1.1419 mL | 2.2839 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。
Comparison of pharmacokinetics between new quinolone antibiotics: the Zabofloxacin hydrochloride capsule and the zabofloxacin aspartate tablet
Curr Med Res Opin 2013 Oct;29(10):1349-55.PMID:23865727DOI:10.1185/03007995.2013.825591
Objectives: Zabofloxacin is being developed as a new fluoroquinolone antibiotic that is a potent and selective inhibitor of the essential bacterial type II topoisomerases and topoisomerase IV. Zabofloxacin is indicated for community-acquired respiratory infections due to Gram-positive bacteria. The aim of this study was to compare the pharmacokinetics (PK) of the Zabofloxacin hydrochloride 400 mg capsule (DW224a, 366.7 mg as zabofloxacin) with the PK of the zabofloxacin aspartate 488 mg tablet (DW224aa, 366.5 mg as zabofloxacin) in healthy Korean male volunteers to assess the bioequivalence between the two drug formulations. Methods: A randomized, open-label, single-dose, two-way crossover study was performed. The subjects received either DW224a or DW224aa according to their sequence group. Plasma concentrations of zabofloxacin were determined by liquid chromatography-tandem mass spectrometry. The maximum plasma concentrations (Cmax), the area under the plasma concentration versus time curve (AUC) from the time of dosing to 48 hours post-dosing (AUClast), and the AUC extrapolated to infinity (AUCinf) were determined from the plasma concentration-time profile. (ClinicalTrials.gov identifier: NCT01341249). Results: Twenty-nine of the 32 subjects enrolled completed the study. The Cmax. AUClast, and AUCinf (mean ± SD) values of DW224a were 1889.7 ± 493.4 ng/mL, 11,110 ± 2,005.0 ng h/mL, and 11,287 ± 2,012.6 ng h/mL, respectively, and those of DW224aa were 2005.0 ± 341.3 ng/mL, 11,719 ± 2,507.5 ng h/mL, and 11,913 ± 2,544.8 ng h/mL, respectively. The geometric mean ratios (90% confidence intervals) of the Cmax. AUClast, and AUCinf were 1.08 (1.00-1.17), 1.05 (1.00-1.10), and 1.05 (1.00-1.10), respectively, and were within the bioequivalence acceptance range of 0.8-1.25. Both drugs were well tolerated with no serious adverse events. Conclusion: A single oral dose of DW224a or DW224aa to healthy volunteers appeared to be well tolerated. Both DW224a and DW224aa exhibited comparable PK profiles and were bioequivalent in terms of PK parameters. Further studies in patients are needed to corroborate the result of this study.