Prulifloxacin
(Synonyms: 普卢利沙星; NM441) 目录号 : GC37020
A prodrug from of ulifloxacin
Cas No.:123447-62-1
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
Prulifloxacin is a prodrug form of the fluoroquinolone antibiotic ulifloxacin.1 In vivo, prulifloxacin increases survival in mouse models of systemic S. aureus, S. pyogenes, S. pneumoniae, E. coli, K. pneumoniae, S. marcescens, or P. aeruginosa infection (ED50s = 0.35-23 mg/kg). It also increases survival in a mouse model of K. pneumoniae-induced respiratory tract infection (ED50 = 0.981 mg/kg).
1.Ozaki, M., Matsuda, M., Tomii, Y., et al.In vivo evaluation of NM441, a new thiazeto-quinoline derivativeAntimicrob. Agents Chemother.35(12)2496-2499(1991)
| Cas No. | 123447-62-1 | SDF | |
| 别名 | 普卢利沙星; NM441 | ||
| Canonical SMILES | O=C(C1=C(SC2C)N2C3=C(C=C(F)C(N4CCN(CC5=C(C)OC(O5)=O)CC4)=C3)C1=O)O | ||
| 分子式 | C21H20FN3O6S | 分子量 | 461.46 |
| 溶解度 | DMSO: 12.5 mg/mL (27.09 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.167 mL | 10.8352 mL | 21.6704 mL |
| 5 mM | 0.4334 mL | 2.167 mL | 4.3341 mL |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.167 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。
Prulifloxacin: a review focusing on its use beyond respiratory and urinary tract infections
Int J Antimicrob Agents 2011 Apr;37(4):283-90.PMID:21300527DOI:10.1016/j.ijantimicag.2010.11.032.
Prulifloxacin is a fluoroquinolone antibiotic that has been approved in several European countries for the treatment of lower urinary tract infections and exacerbations of chronic bronchitis. In this review, PubMed and Scopus databases were searched for potential uses of Prulifloxacin beyond respiratory and urinary tract infections. Nine individual articles (eight randomised controlled trials and one cohort study) were regarded as eligible for inclusion in the review. Three of the studies were double-blinded, whilst six were open-label trials. Three studies referred to the treatment of patients with chronic bacterial prostatitis (CBP), one to prophylaxis of patients undergoing transrectal prostate biopsy, one to prophylaxis of women undergoing surgical abortion, two to patients with traveller's diarrhoea, one to diabetic patients with soft tissue infections or osteomyelitis, and one to improving tolerance of Bacillus Calmette-Guérin (BCG) instillations in patients with bladder cancer. Regarding CBP, Prulifloxacin was non-inferior to its comparators, with a trend towards better microbiological outcomes at follow-up. Regarding traveller's diarrhoea, Prulifloxacin resulted in better clinical and microbiological outcomes compared with placebo. Finally, Prulifloxacin decreased the adverse events associated with BCG instillations in patients with bladder cancer, without affecting cancer recurrence rates. In summary, Prulifloxacin appears to be a promising agent for the treatment of bacterial prostatitis and traveller's diarrhoea.
Prulifloxacin: a new antibacterial fluoroquinolone
Expert Rev Anti Infect Ther 2006 Feb;4(1):27-41.PMID:16441207DOI:10.1586/14787210.4.1.27.
In the last few years, the antimicrobial activity, efficacy and relative safety of fluoroquinolones have made them attractive for the treatment of community-acquired and nosocomial infections. Prulifloxacin is a new fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and -negative bacteria. Prulifloxacin is available for oral use, and after absorption is metabolized in to the active form, ulifloxacin. It exhibits good penetration in target tissues and a long elimination half-life, allowing once-daily administration. A number of randomized, controlled clinical trials carried out in Europe demonstrated the efficacy of Prulifloxacin in the treatment of urinary tract (acute uncomplicated and complicated) and respiratory tract infections (acute exacerbations of chronic bronchitis), in comparison with the most widely used drugs such as ciprofloxacin, co-amoxiclav and pefloxacin. Prulifloxacin was generally well tolerated. The most frequent adverse reactions observed in clinical trials were gastric pain, diarrhea, nausea and skin rash. This review focuses on the characteristics of Prulifloxacin, summarizing the relevant preclinical and clinical data.
Prulifloxacin: clinical studies of a broad-spectrum quinolone agent
Future Microbiol 2009 Feb;4(1):13-24.PMID:19207096DOI:10.2217/17460913.4.1.13.
Prulifloxacin, the lipophilic prodrug of ulifloxacin, is a new oral fluoroquinolone with a broad spectrum of in vitro activity against various Gram-positive and Gram-negative microorganisms. Currently, it is the most potent in vitro fluoroquinolone against Escherichia coli and Pseudomonas aeruginosa, and also has the lowest potential of inducing the emergence of resistant strains for these bacteria. It exhibits good penetration in target tissues and fluids, and possesses a long half-life, thus allowing for once-daily administration. Prulifloxacin has been successfully tested in Phase III randomized, controlled trials including patients with acute exacerbations of chronic bronchitis, uncomplicated and complicated urinary tract infections, and chronic bacterial prostatitis. Results are awaited from recently completed and ongoing Phase III randomized, placebo-controlled studies testing Prulifloxacin for the treatment of traveler's diarrhea. Prulifloxacin has an acceptable toxicity profile, comparable to that of other fluoroquinolones, with gastric disturbances, diarrhea, nausea and skin rash of mild-to-moderate severity being the most frequent adverse events. Additional research is needed to further elucidate the promising role of Prulifloxacin in the treatment of infections sustained by multidrug-resistant pathogens and to consolidate the wide spectrum of activity from a clinical standpoint.
Prulifloxacin
Drugs 2004;64(19):2221-34; discussion 2235-6.PMID:15456336DOI:10.2165/00003495-200464190-00005.
Prulifloxacin, the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. After absorption, Prulifloxacin is metabolised by esterases to ulifloxacin. The drug has a long elimination half-life, allowing once-daily administration. Ulifloxacin is generally more active in vitro than other fluoroquinolones against a variety of clinical isolates of Gram-negative bacteria, including community and nosocomial isolates of Escherichia coli, Klebsiella spp., Proteus, Providencia and Morganella spp., Moraxella catarrhalis and Haemophilus spp. The activity of ulifloxacin against Pseudomonas aeruginosa varies between countries. Gram-positive organisms, including meticillin- or oxacillin-susceptible Staphylococcus aureus, Enterococcus spp. and Italian community isolates of Streptococcus pneumoniae are susceptible to ulifloxacin. Activity against Spanish strains of S. pneumoniae is moderate. In well designed clinical trials, good clinical and bacteriological efficacy (similar to that of ciprofloxacin, amoxicillin/clavulanic acid or pefloxacin) was seen with Prulifloxacin 600 mg once daily for 10 days in patients with acute exacerbations of chronic bronchitis or complicated lower urinary tract infections (UTIs), and with single-dose Prulifloxacin 600 mg in acute, uncomplicated lower UTIs. Prulifloxacin was generally well tolerated in clinical trials, with a similar tolerability profile to that of ciprofloxacin.
Prulifloxacin: a new fluoroquinolone for the treatment of acute exacerbation of chronic bronchitis
Pulm Pharmacol Ther 2006;19 Suppl 1:30-7.PMID:16359895DOI:10.1016/j.pupt.2005.09.007.
Empiric therapy with oral antibiotics is normal practice in the treatment of acute exacerbations of chronic bronchitis (AECB), but there is growing concern regarding efficacy of the currently available antimicrobials. Prulifloxacin, the lipophilic prodrug of ulifloxacin, is an oral fluoroquinolone antibacterial agent with a broad-spectrum in vitro activity against Gram-negative and -positive bacteria, and a long elimination half-life, which allows the once-daily administration. In addition, it penetrates extensively into lung tissues. Statistical analyses indicated a significant linear trend between the Prulifloxacin 300, 450, and 600 mg doses, which would point to an interesting relationship between dose employed and response obtained. The 600 mg once-daily dose showed the best risk/benefit ratio, and was selected for use in the pivotal clinical trials. In well-designed clinical trials, Prulifloxacin 600 mg administered once daily for 10 days in patients with AECB showed good clinical and bacteriological efficacy (similar to that of ciprofloxacin or co-amoxiclav). In particular, the clinical response rates were favourable in all clinical trials, with eradication rates in patients with pneumococcal infections at least as high as the comparators. It can be concluded that Prulifloxacin 600 mg once daily is a new therapeutic prospect in the antimicrobial therapy of AECB. In particular, since good patient compliance is a key factor in the successful treatment of any infection, the once daily treatment with Prulifloxacin may have some compliance advantages compared to the twice-daily treatment with agents such as ciprofloxacin or co-amoxiclav.