Irloxacin
(Synonyms: 伊洛沙星,Pirfloxacin) 目录号 : GC64587
Irloxacin (Pirfloxacin) 是一种喹诺酮类抗菌剂。在酸性条件下，Irloxacin 表现出更大的活性。Irloxacin 对革兰氏阳性菌和革兰氏阴性菌都具有良好的体外抗菌谱。具有口服活性。
Cas No.:91524-15-1
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
Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active[1].
[1]. Casal M, et al. Preliminary study of the in vitro activity of irloxacin against mycobacteria. Chemotherapy. 1995;41(3):204-207. [2]. GuzmÁn A, et al. Acute and subchronic toxicity studies of the new quinolone antibacterial agent irloxacin in rodents. Arzneimittelforschung. 1999;49(5):448-456.
| Cas No. | 91524-15-1 | SDF | Download SDF |
| 别名 | 伊洛沙星,Pirfloxacin | ||
| 分子式 | C16H13FN2O3 | 分子量 | 300.28 |
| 溶解度 | 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 | 3.3302 mL | 16.6511 mL | 33.3023 mL |
| 5 mM | 0.666 mL | 3.3302 mL | 6.6605 mL |
| 10 mM | 0.333 mL | 1.6651 mL | 3.3302 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。
In vitro activities of Irloxacin and E-3846, two new quinolones
Antimicrob Agents Chemother 1990 Jun;34(6):1262-7.PMID:2393288DOI:10.1128/AAC.34.6.1262.
Irloxacin and E-3846 are two new fluorinated quinolones. We evaluated the activities of these antimicrobial agents, ciprofloxacin, ofloxacin, enoxacin, pefloxacin, norfloxacin, and nalidixic acid against 1,161 bacterial strains. Ciprofloxacin was the most active quinolone. Irloxacin did not show great activity. The activity of E-3846 against gram-negative bacteria was similar to those of ofloxacin and pefloxacin, and E-3846 was the most active quinolone against gram-positive bacteria and anaerobes.
Preliminary study of the in vitro activity of Irloxacin against mycobacteria
Chemotherapy 1995 May-Jun;41(3):204-7.PMID:7656667DOI:10.1159/000239345.
Today Mycobacterium avium and Mycobacterium tuberculosis multidrug resistance are responsible for frequent and severe infections in humans and especially in AIDS patients. Irloxacin is a new quinolone derivative, and shows greater activity with an acid pH. It has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. We have compared the in vitro activity of Irloxacin against mycobacteria (20 M. tuberculosis, 17 M. avium, 5 Mycobacterium bovis, 5 Mycobacterium chelonae, 5 Mycobacterium fortuitum and 1 Mycobacterium gadium) using the Bactec at pH 6.8 and 5.0, with other quinolones (ofloxacin, ciprofloxacin, pefloxacin and 27753 RP). All quinolones tested showed good activity against mycobacteria at pH 6.8 and 5.0. Irloxacin at pH 5.0 had a greater activity against M. avium.
Subchronic toxicity of the new quinolone antibacterial agent Irloxacin in beagle dogs
Arzneimittelforschung 2000 May;50(5):485-94.PMID:10858877DOI:10.1055/s-0031-1300234.
The subchronic oral toxicity of the new quinolone antibacterial agent Irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1,4-dihydro-4-oxo-quinolone- 3-carboxylic acid, CAS 91524-15-1) in Beagle dogs was investigated in studies of 4 and 29 weeks of duration. In both studies animals received dosages of 10, 120 and 1400 mg/kg/d. Pale coloured faeces were seen on animals receiving 1400 mg/kg/d. Animals receiving 1400 mg/kg/d for 29 weeks showed an increased incidence of wax in the ears during the latter half of the treatment period, and one male and one female experienced transitory locomotive difficulties at the end of the first week of treatment. The liver was identified as the target organ for toxicity with presence of lipofuscin in the hepatocytes of animals receiving 120 or 1400 mg/kg/d for 29 weeks. Slight increases in liver weights were observed in animals receiving 120 or 1400 mg/kg/d for 4 weeks, and in all groups receiving Irloxacin for 29 weeks. However, no histopathological findings were observed in the liver of animals receiving Irloxacin for 4 weeks or those receiving 10 mg/kg/d for 29 weeks. Other relevant findings observed in the 29 week study were increased triglyceride, phospholipid and cholesterol levels in males receiving 120 mg/kg/d and animals receiving 1400 mg/kg/d, increased albumin and decreased beta-globulin concentrations in females receiving 1400 mg/kg/d, and prolonged activated partial thromboplastin time in animals receiving 1400 mg/kg/d. On the basis of the results obtained it is concluded that 10 mg/kg/d can be considered as the non-toxic dose after 29 week oral administration of Irloxacin in dogs.
Developmental toxicity studies of the quinolone antibacterial agent Irloxacin in rats and rabbits
Arzneimittelforschung 2003;53(2):121-5.PMID:12642968DOI:10.1055/s-0031-1297082.
Embryotoxicity studies on Irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1,4-dihydro-4-oxo-quinolone-3-carboxylic acid, CAS-91524-15-1), a new fluoroquinolone antibacterial agent, were performed in rats and rabbits. Oral administration of Irloxacin during the fetal period of organogenesis to pregnant rats and rabbits at dose levels of up to 1000 and 350 mg/kg/d, respectively, elicited no evidence of teratogenicity. During the first days of treatment, transient stasis in body weight increase was observed in rat dams receiving doses of 350 or 1000 mg/kg/d, and reduced food consumption was observed in those receiving 1000 mg/kg/d. Necropsy on day 20 of gestation showed dosage related increase in liver and kidney weights in all rat treated groups. Rabbit dams receiving 350 mg/kg/d showed during the first days of treatment decrease in body weight, and decreased food consumption and faecal output. Also, four females receiving 350 mg/kg/d aborted between days 18 and 20 of gestation. Rat fetuses in the 350 and 1000 mg/kg/d showed decreased body weight, and a decrease in placental weights was observed in the 1000 mg/kg/d group. No retardations or malformations were observed in rat or rabbit fetuses at any tested dose level. For maternal and embryo-fetal effects 100 and 150 mg/kg/d can be considered as the no-effect-level (NOEL) for rats and rabbits, respectively.
Acute and subchronic toxicity studies of the new quinolone antibacterial agent Irloxacin in rodents
Arzneimittelforschung 1999 May;49(5):448-56.PMID:10367108DOI:10.1055/s-0031-1300441.
Irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1, 4-dihydro-4-oxo-quinolone-3-carboxylic acid, CAS 91524-15-1), a new quinolone antibacterial agent, was administered as a single dose to rats and mice both by oral and intraperitoneal route in oder to study its acute toxicity. Its oral subchronic toxicity was also assessed by treating rats for 4 and 13 weeks. The results obtained showed that Irloxacin was well tolerated after single administration in mice and rats, with LD50 values above 2000 and 5000 mg/kg for intraperitoneal and oral administration, respectively. In the oral subchronic toxicity studies, the histopathological examination performed after the 13-week treatment period confirmed the kidney as the target organ for toxicity. Increased presence of lipofuscin in the kidneys was observed in animals receiving 2000 or 450 mg/kg/d, and degeneration and/or dilatation of proximal renal tubules and chronic interstitial nephritis in males receiving these dosages. No histopathological findings were observed in the kidneys of animals receiving 100 mg/kg/d for 13 weeks. Other relevant findings were, presence of dark or cloudy urine with slightly lower pH in animals receiving dosages of 450 mg/kg/d and above, increased urinary protein concentration in animals receiving 2000 or 450 mg/kg/d, and increased plasma urea concentration in those receiving 2000 mg/kg/d. Moreover, increased plasma phospholipids and total cholesterol concentration, and increased liver and kidney weights were observed among treated animals. As a summary, the results have shown that Irloxacin has a low acute toxicity in both mice and rats. For repeat oral administration in rats, 100 mg/kg can be considered as the non-toxic effect level after a treatment period of 13 weeks.