Trovafloxacin
(Synonyms: 曲伐沙星) 目录号 : GC60374
A topoisomerase IV and DNA gyrase inhibitor
Cas No.:147059-72-1
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
Trovafloxacin is a broad spectrum antibiotic that inhibits the uncoiling of supercoiled DNA in bacteria by blocking the activity of topoisomerase IV (IC50 = 3.02 ?g/ml) and DNA gyrase (IC50 = 7.13 ?g/ml).1
1.Takei, M., Fukuda, H., Kishii, R., et al.Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibitionAntimicrob. Agents Chemother.45(12)3544-3547(2001)
| Cas No. | 147059-72-1 | SDF | |
| 别名 | 曲伐沙星 | ||
| Canonical SMILES | O=C(C1=CN(C2=CC=C(F)C=C2F)C3=NC(N4C[C@@]5([H])[C@H](N)[C@@]5([H])C4)=C(F)C=C3C1=O)O | ||
| 分子式 | C20H15F3N4O3 | 分子量 | 416.35 |
| 溶解度 | DMSO : 10 mg/mL (24.02 mM; ultrasonic and adjust pH to 2 with 1M HCl); DMSO : 9.09 mg/mL (21.83 mM; ultrasonic and adjust pH to 3 with HCl) | 储存条件 | |
| 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 | 2.4018 mL | 12.0091 mL | 24.0183 mL |
| 5 mM | 0.4804 mL | 2.4018 mL | 4.8037 mL |
| 10 mM | 0.2402 mL | 1.2009 mL | 2.4018 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。
Trovafloxacin
Drugs 1997 Sep;54(3):435-45; discussion 446.PMID:9279505DOI:10.2165/00003495-199754030-00006.
Trovafloxacin is a fluoroquinolone antibacterial agent with a broad spectrum of activity. Trovafloxacin has similar or 2-fold lower activity than ciprofloxacin against Enterobacteriaceae and Pseudomonas aeruginosa. Against Haemophilus influenzae and Moraxella catarrhalis, Trovafloxacin has similar activity to ciprofloxacin. Other susceptible Gram-negative pathogens include Neisseria gonorrhoeae, Chlamydia trachomatis and mycoplasmas. The drug is active against Gram-positive bacteria and consistently displayed greater activity (2- to 8-fold) than ciprofloxacin against all staphylococci and streptococci tested; activity included methicillin-resistant staphylococci and penicillin-resistant Streptococcus pneumoniae. Trovafloxacin has some activity against vancomycin-resistant enterococci. Anaerobes such as Bacteroides and Clostridium spp. are also susceptible to Trovafloxacin. Preliminary clinical data suggest that Trovafloxacin is effective in the treatment of patients with upper and lower respiratory tract and uncomplicated urinary tract infections and infections caused by C. trachomatis or N. gonorrhoeae. The most frequently noted adverse event with Trovafloxacin is dizziness which is reported in 11% of patients versus 3% of those receiving comparator agents. Other commonly reported events (> 1% of patients) are nausea, headache, vomiting, vaginitis and diarrhoea.
Trovafloxacin: an overview
Pharmacotherapy 1999 Jan;19(1):21-34.PMID:9917076DOI:10.1592/phco.19.1.21.30507.
Trovafloxacin, a new synthetic naphthyridine fluoroquinolone antibiotic, is a broad-spectrum agent available orally and intravenously. It was recently approved by the Food and Drug Administration for the treatment of selected pulmonary, surgical, intraabdominal, gynecologic, pelvic, skin, and urinary tract infections. Its spectrum of activity includes aerobic gram-positive and gram-negative organisms as well as anaerobic pathogens. It is rapidly absorbed after oral administration, achieves good tissue and cerebrospinal fluid penetration, and has a half-life that allows once-daily dosing. It is hepatically metabolized, and dosage adjustments are necessary for patients with severe hepatic dysfunction but not for those with mild or moderate dysfunction or renal dysfunction. The drug has a favorable safety profile, and a high tendency for transient first-dose dizziness and/or lightheadedness in young women. Similar to other quinolones, Trovafloxacin should not be taken with antacids that contain aluminum or magnesium, sucralfate, or ferrous sulfate. Trovafloxacin may prove beneficial as it allows for oral or intravenous monotherapy against indicated infections that normally require multidrug, broad-spectrum antibiotic coverage.
Trovafloxacin: a new fluoroquinolone
Ann Pharmacother 1999 Jan;33(1):48-60.PMID:9972385DOI:10.1345/aph.17460.
Objective: To review the pharmacology, antimicrobial activity, pharmacokinetics, clinical efficacy, and safety of Trovafloxacin. Data sources: A MEDLINE search (January 1966-April 1998) was conducted for relevant literature using the terms CP-99,219, CP-116,519, Trovafloxacin, and alatrofloxacin. Abstracts published by the American Society of Microbiology during 1995-1997 meetings were also reviewed. Study selection and data extraction: All in vitro, animal, and human studies were reviewed for the antimicrobial activity, pharmacokinetics, efficacy, and safety of Trovafloxacin. Data synthesis: Trovafloxacin is a new fluoroquinolone with enhanced activity against gram-positive and anaerobic microorganisms. The oral bioavailability under fasting conditions is approximately 88%. The elimination half-life of Trovafloxacin is approximately 10 hours. Less than 10% of Trovafloxacin is eliminated unchanged in the urine. Trovafloxacin is effective in the treatment of community-acquired pneumonia and nosocomial pneumonia with cure rates of > 90% and 77%, respectively. Trovafloxacin is comparable with ceftriaxone in the treatment of meningococcal meningitis in children; each produces a cure rate of approximately 90%. In treatment of uncomplicated urinary tract infection, both ciprofloxacin and Trovafloxacin achieve an eradication rate of > or = 93%. Trovafloxacin is similar to ofloxacin in the treatment of urogenital Chlamydia trachomatis and acute exacerbations of chronic bronchitis, with clinical success in 97% of patients with each drug. The common adverse effects of Trovafloxacin include dizziness, headache, and gastrointestinal intolerance. Conclusions: The advantages of once-daily dosing and enhanced activity of Trovafloxacin against gram-positive and anaerobic organisms may expand its use over available fluoroquinolones. Further studies are needed to define its role in the treatment of various infectious diseases.
Levofloxacin and Trovafloxacin: the next generation of fluoroquinolones?
Am J Health Syst Pharm 1997 Nov 15;54(22):2569-84.PMID:9397218DOI:10.1093/ajhp/54.22.2569.
The pharmacology, spectrum of activity, pharmacokinetics, clinical efficacy, and adverse effects of levofloxacin, recently approved by FDA, and Trovafloxacin, currently undergoing clinical trials, are reviewed. Compared with quinolones in current use, levofloxacin is more potent against gram-negative bacteria and exhibits better antipseudomonal activity as well as greater oral bioavailability. Trovafloxacin is more potent than existing quinolones against gram-positive bacteria. Both agents exert their antibacterial effects by inhibiting bacterial DNA synthesis. Compared with other quinolones, levofloxacin and Trovafloxacin both demonstrate superior activity against the Bacteroides fragilis group, Chlamydia spp., Mycoplasma pneumoniae, and Mycobacterium spp. The half-life (t1/2) of levofloxacin is nearly eight hours. Levofloxacin can therefore be administered once daily for mild to moderate infections and twice daily for more serious infections. The recommended daily dose is 500 mg. Trovafloxacin has a t1/2 of 12 hours, which allows for single daily doses, and is extensively metabolized. Levofloxacin has demonstrated clinical efficacy in the treatment of community-acquired respiratory-tract infections, genitourinary infections, skin and skin-structure infections, acute bacterial sinusitis, and infections of the head and neck. Trovafloxacin may have a role in treating skin and skin-structure or soft-tissue infections respiratory-tract infections, sexually transmitted diseases, and meningitis. Both agents are well tolerated, with central-nervous-system and gastrointestinal adverse effects reported most frequently. Concomitant administration of antacids or compounds containing meal cations decreases absorption of these quinolones. Levofloxacin and Trovafloxacin have favorable antimicrobial and pharmacokinetic profiles, offering the advantages of once-daily doses as well as superior potency and spectrum of activity compared with currently available quinolones.
Trovafloxacin-associated leukopenia
Ann Pharmacother 2001 Jan;35(1):41-4.PMID:11197584DOI:10.1345/aph.10066.
Objective: To report a case of trovafloxacin-associated leukopenia, which occurred in a trauma patient shortly after administration and resolved following discontinuation of the drug. Case summary: A 79-year-old white man was admitted to Yale New Haven Hospital after sustaining partial amputation of his right lower leg by an industrial lawn mower. After successful resuscitation, he underwent complete right lower amputation and was treated with intravenous alatrofloxacin mesylate. He developed leukopenia that resolved after discontinuation of the drug. Discussion: Trovafloxacin is a broad-spectrum synthetic fluoroquinolone used for a wide variety of bacterial infections. We report, for the first time in the English-language literature, a case of trovafloxacin-associated leukopenia. The leukopenia resolved promptly after discontinuation of the drug. This association is further supported by the exclusion of other potential causes for this adverse effect. Conclusions: Leukopenia is a well-recognized adverse effect of several drugs. We report a case of trovafloxacin-associated leukopenia during treatment of a trauma patient. Healthcare personnel should be aware of this possible adverse reaction in patients treated with Trovafloxacin.