N-desmethyl Levofloxacin
(Synonyms: 左氧氟沙星相关物质A) 目录号 : GC44349
An active metabolite of levofloxacin
Cas No.:117707-40-1
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
N-desmethyl Levofloxacin is an active metabolite of the fluoroquinolone antibiotic levofloxacin . It is active against S. aureus, S. epidermidis, B. subtilis, E. coli, P. aeruginosa, and K. pneumoniae (MICs = 4, 1, 1, 0.012, >4, and 0.25 μg/ml, respectively).
| Cas No. | 117707-40-1 | SDF | |
| 别名 | 左氧氟沙星相关物质A | ||
| Canonical SMILES | FC1=C(N2CCNCC2)C(OC[C@H](C)N3C=C(C(O)=O)C4=O)=C3C4=C1 | ||
| 分子式 | C17H18FN3O4 | 分子量 | 347.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 5 mg/ml | 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 | 2.8794 mL | 14.3968 mL | 28.7936 mL |
| 5 mM | 0.5759 mL | 2.8794 mL | 5.7587 mL |
| 10 mM | 0.2879 mL | 1.4397 mL | 2.8794 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。
Synthesis and antibacterial activity of novel levofloxacin derivatives containing a substituted thienylethyl moiety
Daru 2012 Aug 30;20(1):16.PMID:23351676DOI:10.1186/2008-2231-20-16.
Background and the purpose of the study: Piperazinyl quinolones such as ciprofloxacin, ofloxacin and levofloxacin are an important group of quinolone antimicrobials which are widely used in the treatment of various infectious diseases. In the present study, we synthesized a new series of levofloxacin derivatives and evaluated their antibacterial activities. Methods: The N-substituted analogs of levofloxacin 6a-j were prepared by nucleophilic reaction of N-desmethyl Levofloxacin 11 with thienylethyl bromide derivatives 8 or 9. All target compounds were tested using conventional agar dilution method in comparison to levofloxacin and N-desmethyl Levofloxacin and their MIC values were determined against a panel of Gram-positive and Gram-negative bacteria. Results: All compounds showed significant antibacterial activities against Gram-positive bacteria (MIC = 0.04-6.25 μg/mL); however, the activity against Gram-negative bacteria was lower (MIC = 1.56-100 μg/mL). As is evident from the data, oxime derivatives 6e, 6h and 6i are superior in inhibiting the growth of Gram-positive bacteria (MIC = 0.04-0.19 μg/mL), and their activities were found to be 5-25 times better than N-desmethyl Levofloxacin 11 and equal or better than levofloxacin 4. Conclusion: We have designed and synthesized novel quinolone derivatives bearing functionalized thienylethyl moiety on the piperazine ring of levofloxacin. The results of antibacterial screening against Gram-positive and Gram-negative bacteria revealed that the introduction of functionalized thienylethyl moiety on the piperazine ring of levofloxacin can improve the activity against Gram-positive bacteria. Gram-positive bacteria are responsible for a wide range of infectious diseases, and rising resistance in this group is causing increasing concern. Thus, this study introduces structural features of levofloxacin scaffold for development of new candidates in the field of anti-Gram positive chemotherapy.
Synthesis and antibacterial activity of nitroaryl thiadiazole-levofloxacin hybrids
Arch Pharm (Weinheim) 2006 Nov;339(11):621-4.PMID:17036368DOI:10.1002/ardp.200600108.
Novel levofloxacin-containing hybrids carrying a 5-(nitroaryl)-1,3,4-thiadiazol-2-yl group were synthesized and evaluated in vitro against Gram-positive and Gram-negative bacteria. Preliminary data indicated that levofloxacin-nitrofuran and levofloxacin-nitroimidazole hybrids have a potent activity against Gram-positive organisms with enhanced anti-staphylococcal activity compared with the parent quinolone (N-desmethyl Levofloxacin).