Temafloxacin
(Synonyms: 替马沙星,TMFX; TA-167 free acid; A-62254 free acid) 目录号 : GC45009
A DNA topoisomerase inhibitor
Cas No.:108319-06-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Temafloxacin is a fluoroquinolone antibiotic that acts as a DNA topoisomerase inhibitor. It has broad antimicrobial activity against gram-positive and gram-negative bacteria, such as S. pneumoniae, M. hominis, and anaerobic bacteria, including B. fragilis.
| Cas No. | 108319-06-8 | SDF | |
| 别名 | 替马沙星,TMFX; TA-167 free acid; A-62254 free acid | ||
| Canonical SMILES | CC1CN(C2=C(F)C=C(C(C(C(O)=O)=CN3C4=CC=C(F)C=C4F)=O)C3=C2)CCN1 | ||
| 分子式 | C21H18F3N3O3 | 分子量 | 417.4 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 2 mg/ml,PBS (pH 7.2): 0.5 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 | 2.3958 mL | 11.9789 mL | 23.9578 mL |
| 5 mM | 0.4792 mL | 2.3958 mL | 4.7916 mL |
| 10 mM | 0.2396 mL | 1.1979 mL | 2.3958 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。
Temafloxacin: an overview
Am J Med 1991 Dec 30;91(6A):166S-172S.PMID:1662889DOI:10.1016/0002-9343(91)90332-r.
Temafloxacin (6-fluoro-7-piperazino-4-quinolone) is a new fluoroquinolone with a 7-8 hour half-life and rapid gastrointestinal absorption. These characteristics make it an ideal antimicrobial for once- or twice-daily oral dosing. With the exception of the central nervous system (CNS), Temafloxacin has excellent tissue and body fluid penetration and concentration. Temafloxacin has broad antimicrobial activity against gram-positive and gram-negative bacteria, including improved in vitro activity against Streptococcus pneumoniae, Mycoplasma hominis, and anaerobic bacteria, including Bacteroides fragilis. Temafloxacin is as effective as beta-lactam therapy and superior to ciprofloxacin in the treatment of S. pneumoniae lower respiratory infections. It has been clinically effective when given in a short 3-day regimen for the treatment of uncomplicated urinary tract infections. Multiple clinical trials indicate that Temafloxacin is also clinically effective, well tolerated, and safe for use in adult patients for the treatment of other lower respiratory tract, genitourinary tract, and skin and skin-structure infections.
Evaluation of the bactericidal activity of Temafloxacin
Am J Med 1991 Dec 30;91(6A):31S-34S.PMID:1662893DOI:10.1016/0002-9343(91)90307-j.
Although the fluoroquinolones share many properties, these agents differ in their ability to kill the same bacterial strain. The bactericidal activity of Temafloxacin against a number of pathogens has been compared with that of other fluoroquinolones by determination of minimal bactericidal concentration, time-kill kinetics, and postantibiotic effect. Studies have demonstrated that Temafloxacin has equivalent or superior ability to kill when compared with other fluoroquinolones. Temafloxacin, ciprofloxacin, and PD 117558 were more active than other fluoroquinolones against Mycobacterium avium complex, with 90% minimal bactericidal concentrations (MBC90S; 8-16 micrograms/mL) four- to eightfold greater than 90% minimal inhibitory concentrations (MIC90S; 2 micrograms/mL). Against Chlamydia trachomatis the MIC90 and MBC90 of Temafloxacin were both 0.25 microgram/mL; ciprofloxacin was less active (MBC90 twice the MIC90), and norfloxacin was least active. Temafloxacin demonstrated more rapid killing kinetics than did ciprofloxacin or ofloxacin at all concentrations tested against Streptococcus pyogenes. Findings were similar against Streptococcus pneumoniae at antibiotic concentrations of 1-2 micrograms/mL. Similar time-kill curves against Escherichia coli were observed for Temafloxacin, ciprofloxacin, and difloxacin. Time-kill kinetics of Temafloxacin against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive S. aureus (MSSA) were superior to those of ciprofloxacin and ofloxacin. Postantibiotic effect with Temafloxacin against Legionella pneumophila showed a considerable delay in regrowth, and Temafloxacin delayed regrowth of MRSA and MSSA to a greater extent than did ciprofloxacin or ofloxacin. By the three methods used in the studies to assess bactericidal activity that are currently published, Temafloxacin had equivalent or superior activity to the comparative fluoroquinolones tested. Other organisms remain to be tested and the significance of these findings determined in clinical studies.
Comparative pharmacokinetics of ciprofloxacin and Temafloxacin in humans: a review
Am J Med 1991 Dec 30;91(6A):51S-66S.PMID:1662896DOI:10.1016/0002-9343(91)90312-l.
Temafloxacin is a new antibacterial agent of the fluoroquinolone group. In comparison with ciprofloxacin, the current leading quinolone, Temafloxacin shows higher and longer lasting plasma concentrations after equivalent doses due to an almost complete gastrointestinal absorption and a lower total clearance. Temafloxacin absorption is little influenced by food intake. Concomitant administration of antacids should be avoided; a time interval of at least 2 hours should elapse between intake of either quinolone and an antacid. Both quinolones are excreted mainly by the kidney. They differ in tubular secretion, which is high for ciprofloxacin and low for Temafloxacin. The overall nonrenal elimination is similar for both compounds. Ciprofloxacin has a slightly higher extent of metabolism, while Temafloxacin probably has a higher transintestinal elimination. The biliary excretion of both compounds is in the same range. The longer half-life of Temafloxacin enables a once-daily dose regimen, whereas the usual recommended dosage of ciprofloxacin is twice daily. For both quinolones the apparent volumes of distribution per body weight are significantly above unity, indicating good tissue penetration with intracellular uptake. The concentrations in the extracellular fluids are directly related to the corresponding plasma concentrations. The penetration of Temafloxacin into the body fluids investigated--tears, nasal secretion, saliva, sweat, prostatic and seminal fluid--in general exceeds that of ciprofloxacin (with the exception of seminal fluid). Unlike ciprofloxacin, there is no drug interaction with methylxanthines. Comparative clinical studies reflecting the complex interrelating factors of host and pathogens are needed to demonstrate the significance of the pharmacokinetic differences between Temafloxacin and ciprofloxacin.
The role of Temafloxacin in the community setting: an overview
J Antimicrob Chemother 1991 Dec;28 Suppl C:121-30.PMID:1664825DOI:10.1093/jac/28.suppl_c.121.
The use of new quinolones has become established therapy for many community infections including urinary tract infection, genital infection, soft tissue infection and some forms of lower respiratory tract infection. However, there has been an undercurrent of anxiety concerning their efficacy in pneumococcal infections. Temafloxacin has improved activity against pneumococci and its high oral bioavailability and excellent penetration into respiratory tissues now combine to provide a suitable profile for the management of a wider range of respiratory infections. Eradication rates in acute exacerbations of chronic bronchitis collated from individual studies are 98% overall and 100% in pneumococcal infections. Furthermore, eradication rates in smokers and the elderly illustrate significant advantages for Temafloxacin when compared with previous quinolones. In pneumonia, a twice-daily Temafloxacin regimen has given equivalent overall results to those of amoxycillin (84.6% vs 80%). In proven pneumococcal pneumonia, equivalent results (78.6% vs 78.4%) have been obtained with both drugs. A daily 600 mg dose of Temafloxacin eradicated 94% of pneumococcal isolates in one study and in another this agent given twice-daily orally proved comparable to parenteral cephalosporin treatment. Temafloxacin shares with other quinolones excellent bacteriological and clinical efficacy against Haemophilus influenzae and Moraxella catarrhalis. These results and the lack of potential interaction with theophylline indicate Temafloxacin to be suitable for domiciliary management of respiratory tract infections in addition to a broad range of other community infectious diseases.
Temafloxacin syndrome: review of 95 cases
Clin Infect Dis 1994 Jun;18(6):946-50.PMID:8086558DOI:10.1093/clinids/18.6.946.
Four months after its approval in the United States, Temafloxacin was withdrawn from the market worldwide because of frequent reports of serious hemolysis with or without other organ system dysfunction. We describe this "Temafloxacin syndrome" on the basis of a review of 95 spontaneous reports of hemolysis sent to the Food and Drug Administration. Patients typically presented with fever, chills, and jaundice a mean of 6.4 days after starting therapy. A moderate degree of hemolysis was reflected by the mean drop in hemoglobin level (by 42 g/L) and by the mean lowest concentration of hemoglobin (97 g/L). New-onset renal dysfunction was noted in 54 cases (57%), and dialysis was required in 34 cases (63%). Coagulopathy was noted in 33 cases (35%), and 48 cases (51%) met the criteria for hepatic dysfunction. Four patients developed central nervous system complications, and two patients died. Prior quinolone use was more common among patients who developed hemolysis after only one dose as opposed to two or more doses (P < .001). These data suggest that Temafloxacin causes immune hemolytic anemia, most likely secondary to immune complex formation.