Amifloxacin (Win49375)
(Synonyms: 氨氟沙星; Win49375) 目录号 : GC33997
Amifloxacin (Win49375) is a fluorinated quinolone-carboxylic acid antibacterial agent with activity against a broad range of gram-negative organisms.
Cas No.:86393-37-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Animal experiment [1]: | |
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Animal models |
ICR female mice weighing 18 to 20 g |
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Preparation Method |
ICR female mice were inoculated intraperitoneally with 0.5 ml of the E. coli Vogel bacterial suspension and then distributed into subgroups of 10 to receive serial twofold doses of the test agents and a subgroup of 20 to serve as untreated controls. The infected mice were medicated p.o. 0.8-1.3 mg/kg or s.c. 0.2-1.6 mg/kg of Amifloxacin (Win49375). The number of survivors was determined daily for 7 days. |
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Dosage form |
0.8-1.3 mg/kg/d for 7 days, p.o.; 0.2-1.6 mg/kg/d for 7 days, s.c. |
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Applications |
Amifloxacin (Win49375) showed a consistently high protective effect against bacterial infection, with ED50s of 1.0 mg/kg for p.o. and 1.0 mg/kg for s.c. . |
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References: [1]: Cornett J B, Wagner R B, Dobson R A, et al. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin)[J]. Antimicrobial agents and chemotherapy, 1985, 27(1): 4-10. | |
Amifloxacin (Win49375) is a fluorinated quinolone-carboxylic acid antibacterial agent with activity against a broad range of gram-negative organisms. The MICs for 90% of isolates of representative urinary tract pathogens are 0.125μg/ml for Escherichia coli, 0.5μg/ml for Klebsiella pneumoniae, 1.0ug/ml for Proteus vulgaris, 0.5ug/ml for Citrobacter freundii, 2.0μg/ml for Pseudomonas aeruginosa, and 0.5ug/ml for Serratia marcescens [1].
Amifloxacin (Win49375), was an effective drug against experimental infections in mice when given parenterally. Amifloxacin (Win49375) was highly active by the oral route, with 50% effective doses within two- to three fold of those obtained with parenteral medication [2].
References:
[1]. Neu H C, Labthavikul P. Antibacterial activity of amifloxacin (WIN 49, 375), a new quinolone agent[J]. Diagnostic microbiology and infectious disease, 1985, 3(6): 469-478.
[2]. Cornett J B, Wagner R B, Dobson R A, et al. In vitro and in vivo antibacterial activities of the fluoroquinolone WIN 49375 (amifloxacin)[J]. Antimicrobial agents and chemotherapy, 1985, 27(1): 4-10.
Amifloxacin (Win49375) 是一种氟化喹诺酮羧酸类抗菌剂，对多种革兰氏阴性菌具有活性。 90% 的代表性尿路病原体分离株的 MIC 为大肠杆菌 0.125μg/ml，肺炎克雷伯菌 0.5μg/ml，普通变形杆菌 1.0ug/ml，弗氏柠檬酸杆菌 0.5ug/ml，弗氏柠檬酸杆菌 2.0μg/ml铜绿假单胞菌和粘质沙雷氏菌 0.5ug/ml [1].
Amifloxacin (Win49375) 是一种有效的药物，当通过胃肠外给药时，它可以有效对抗小鼠的实验性感染。阿米沙星 (Win49375) 在口服途径中具有很高的活性，50% 的有效剂量是肠胃外用药的两到三倍[2]。
| Cas No. | 86393-37-5 | SDF | |
| 别名 | 氨氟沙星; Win49375 | ||
| Canonical SMILES | O=C(C1=CN(NC)C2=C(C=C(F)C(N3CCN(C)CC3)=C2)C1=O)O | ||
| 分子式 | C16H19FN4O3 | 分子量 | 334.35 |
| 溶解度 | Soluble in DMSO | 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 | 2.9909 mL | 14.9544 mL | 29.9088 mL |
| 5 mM | 0.5982 mL | 2.9909 mL | 5.9818 mL |
| 10 mM | 0.2991 mL | 1.4954 mL | 2.9909 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。
Amifloxacin activity against well-defined gentamicin-resistant, gram-negative bacteria
Antimicrob Agents Chemother.1984 Nov;26(5):781-4.PMID: 6440481 DOI: 10.1128/AAC.26.5.781
Amifloxacin (WIN 49375) activity against a well-defined group of gentamicin-resistant gram-negative bacilli was compared with the activity of 11 other antimicrobial agents. For all strains, amifloxacin and norfloxacin were the most active agents, followed by cefotaxime and moxalactam. For Acinetobacter sp. only amifloxacin had an achievable MIC for 90% of the strains. Amifloxacin joins other newly developed DNA gyrase inhibitors as potentially useful agents for infections due to aminoglycoside-resistant gram-negative bacilli.
In vitro activities of amifloxacin and two of its metabolites
Antimicrob Agents Chemother.1989 May;33(5):762-6. PMID: 2751287DOI: 10.1128/AAC.33.5.762
Amifloxacin and two of its metabolites, N-desmethyl amifloxacin and amifloxacin N-oxide, were evaluated by a microdilution MIC susceptibility test against 500 clinical isolates and compared with ciprofloxacin, lomefloxacin, norfloxacin, aztreonam, and imipenem. Of the Staphylococcus species isolates, 208 were methicillin resistant; the MICs for 78 of the isolates of the family Enterobacteriaceae were greater than or equal to 64 micrograms of cefazolin, ampicillin, piperacillin, and mezlocillin per ml. Based on our results, amifloxacin had activity equivalent to those of norfloxacin and lomefloxacin but was less active than ciprofloxacin. The N-oxide metabolite was the least active; however, for the majority of gram-negative bacteria, N-desmethyl amifloxacin was as active as amifloxacin.
Multiple-dose pharmacokinetics and safety of oral amifloxacin in healthy volunteers
Antimicrob Agents Chemother1990 Jun;34(6):974-9.PMID: 2393295DOI: 10.1128/AAC.34.6.974
The multiple-dose pharmacokinetics and safety of amifloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy male volunteers. Amifloxacin was administered orally at 200, 400, or 600 mg every 12 h (q12h) and 400, 600, or 800 mg every 8 h (q8h) for 10 days. An additional dose was administered on day 11. Concentrations of amifloxacin in plasma and urine were measured on days 1, 5, and 11 by high-performance liquid chromatography. Steady-state amifloxacin concentrations were reached by day 5. Mean +/- standard deviation maximum observed amifloxacin concentrations in plasma were 2.52 +/- 1.12, 4.98 +/- 1.44, 5.40 +/- 2.02, 4.59 +/- 2.17, 6.53 +/- 2.44, and 8.01 +/- 3.00 micrograms/ml after the initial dose and 2.30 +/- 0.98, 5.41 +/- 0.74, 8.05 +/- 1.68, 6.87 +/- 2.81, 9.53 +/- 0.50, and 11.9 +/- 1.92 micrograms/ml on day 11 of the study for the 200-, 400-, and 600-mg q12h and 400-, 600-, and 800-mg q8h regimens, respectively. Amifloxacin was rapidly absorbed, as evidenced by the mean time to the maximum observed amifloxacin concentration of 0.98 h. Mean values for the terminal amifloxacin half-life in plasma ranged from 3.58 to 5.78 h. Mean amifloxacin concentrations in urine on day 11 in samples collected 0 to 2 h after dosing were 105, 417, 376, 336, 518, and 464 micrograms/ml for the 200-, 400-, and 600-mg q12h and 400-, 600-, and 800-mg q8h regimens, respectively. The mean amount of the dose excreted in the urine as amifloxacin was 53.9%. Amifloxacin was generally well tolerated, although there was a tendency for the subjects who received amifloxacin to experience more gastrointestinal, central nervous system, and cutaneous complaints than did those who received placebo. Clinically significant adverse reactions, including pruritus and transaminase elevations, occurred only at doses of 1,200 mg/day or above. Clinical and pharmacokinetic data suggest that orally administered amifloxacin may have utility in the treatment of urinary tract infections.
Metabolism and disposition of amifloxacin in laboratory animals
Antimicrob Agents Chemother.1985 May;27(5):774-81.PMID: 4015071DOI: 10.1128/AAC.27.5.774
Sprague-Dawley rats received [14C]amifloxacin mesylate either orally or intravenously at 20 mg (base equivalent) per kg. Blood radioactivity peaked at 0.5 h after oral administration and was equivalent to 7.54 micrograms/ml for males and 6.73 micrograms/ml for females. After intravenous administration to rats, 52.5% of the dose was recovered in the urine of males and 45.3% in the urine of females within 72 h. The corresponding values after oral administration were 50.8% for males and 37.2% for females. The remainder of the dose was recovered in the feces. After intravenous administration of [14C]amifloxacin mesylate at 10 mg (base equivalent) per kg to female rhesus monkeys, 80.3% of the radioactivity was excreted in the urine at 24 h. The apparent first-order terminal elimination half-life of intact amifloxacin in plasma was 2.3 h; radioactivity in plasma was eliminated more slowly. Male rats excreted 26.2% of the dose in the urine as amifloxacin and 17.8% as the piperazinyl-N-oxide derivative of amifloxacin after intravenous administration. The corresponding amounts for female rats were 29.0% as amifloxacin and 7.8% as the piperazinyl-N-oxide metabolite. Similar excretion profiles were observed after oral administration. After intravenous administration, female monkeys excreted 54.5% of the dose in the urine as amifloxacin, 12.9% as the piperazinyl-N-desmethyl metabolite, and 5.6% as the piperazinyl-N-oxide during the first 12 h. In contrast, there was no evidence of the piperazinyl-N-desmethyl metabolite in rats.
Antibacterial activity of amifloxacin (WIN 49, 375), a new quinolone agent
Diagn Microbiol Infect Dis.1985 Nov;3(6):469-78.PMID: 4064609 DOI: 10.1016/s0732-8893(85)80003-1 Abstract
The in vitro activity of amifloxacin, a quinolone antimicrobial agent was compared with those of ciprofloxacin, enoxacin, ofloxacin and norfloxacin against gram-positive and gram-negative bacteria. Ninety percent of Escherichia coli, Klebsiella species, Aeromonas, Salmonella, Shigella, Citrobacter, Enterobacter species, Proteus mirabilis, Serratia marcescens, and Morganella morganii were inhibited by less than or equal to 0.5 microgram/ml. Amifloxacin inhibited Branhamella, Haemophilus, and Neisseria at less than or equal to 0.25 microgram/ml, and 90% of Pseudomonas aeruginosa, including gentamicin- and carbenicillin-resistant isolates, at 4 micrograms/ml. It also inhibited staphylococci, including methicillin-resistant isolates, but was less active against streptococci and Bacteroides species. Amifloxacin had in vitro activity similar to enoxacin, ofloxacin, and norfloxacin, but was less active than ciprofloxacin. Like other quinolones, it was less active at acid pH and in the presence of urine.