Aspoxicillin
(Synonyms: 阿扑西林) 目录号 : GC63886
Aspoxicillin 是一种广谱的抗菌剂，对分离的胸膜肺炎放线杆菌 68 菌株抑制作用的 MIC90 值 <= 0.05 μg/ml。Aspoxicillin 在小鼠血清中的半衰期为 55 分钟。
Cas No.:63358-49-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Aspoxicillin is a broad-spectrum antimicrobial agent against 68 isolates of Actinobacillus pleuropneumoniae with an MIC90 value of <= 0.05 μg/ml. Aspoxicillin has a long half-life in mouse serum of 55 minutes[1][2].
Aspoxicillin is a semisynthetic penicillin derivative[2]Aspoxicillin induces postantibiotic effects (PAEs) against Staphylococcus aureus Smith of 1.7 h in vitro[2].
Aspoxicillin induces PAEs against Staphylococcus aureus Smith of 5.2 h in vivo in a thigh infection model in neutropenic mice[2].
[1]. Yoshimura H, et al. Comparative in vitro activity of 16 antimicrobial agents against Actinobacillus pleuropneumoniae. Vet Res Commun. 2002 Jan;26(1):11-9.
[2]. Oshida T, et al. Activity of sub-minimal inhibitory concentrations of aspoxicillin in prolonging the postantibiotic effect against Staphylococcus aureus. J Antimicrob Chemother. 1990 Jul;26(1):29-38.
| Cas No. | 63358-49-6 | SDF | Download SDF |
| 别名 | 阿扑西林 | ||
| 分子式 | C21H27N5O7S | 分子量 | 493.53 |
| 溶解度 | Water : 25 mg/mL (50.66 mM; Need ultrasonic) | 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 | 2.0262 mL | 10.1311 mL | 20.2622 mL |
| 5 mM | 0.4052 mL | 2.0262 mL | 4.0524 mL |
| 10 mM | 0.2026 mL | 1.0131 mL | 2.0262 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。
Aspoxicillin versus piperacillin in severe abdominal infections--a comparative phase III study
J Antimicrob Chemother 1994 Nov;34(5):813-7.PMID:7706179DOI:10.1093/jac/34.5.813.
We compared Aspoxicillin, a new broad-spectrum penicillin derivative, with piperacillin in severe abdominal infection. Aspoxicillin 4 g administered tds (n = 52) or piperacillin 4 g qds (n = 53) usually as monotherapy were randomly given to patients suffering from perforated appendicitis, acute cholecystitis, ulcer or colon perforation, or intra-abdominal abscess. Blood, tissue and exudate cultures were obtained when applicable for pathogen identification and susceptibility testing. The efficacy rates were similar in the two study groups. Of the 50 evaluable Aspoxicillin patients 45 (90%) were considered as treatment responders compared with 48 patients out of 53 (91%) in the piperacillin group (NS). The 95% confidence interval for the efficacy difference was -12% to +11% thus showing no difference between the two drugs. Both drugs were generally well tolerated and no serious drug-related adverse events were noted. However, five patients died because of their illness and one patient had a fatal myocardial infarction. In conclusion, Aspoxicillin 4 g tds was shown to be equal to piperacillin 4 g qds in severe abdominal infections.
[Review: New antimicrobial agent series XXII: Aspoxicillin]
Jpn J Antibiot 1987 Jul;40(7):1221-42.PMID:3316732doi
The results of clinical and laboratory studies on Aspoxicillin (ASPC) are summarized in this paper. 1. ASPC possesses a broad antibacterial spectrum in vitro against Gram-positive and Gram-negative bacteria. ASPC shows more potent activity in vivo and stronger bactericidal action than expected from in vitro activity. 2. Peak blood levels of ASPC after intravenous injection or intravenous drip infusion are dose dependent and half-lives of ASPC in these cases are about 1.6 hours. ASPC is excreted in active form mostly into urine via kidney. ASPC is satisfactorily transferred into various tissues and body fluids, such as bile, sputum. The binding rate of ASPC to serum protein is much lower than penicillin derivatives like piperacillin (PIPC), sulbenicillin (SBPC) and ampicillin (ABPC). 3. In an open clinical trial of ASPC, 1,845 cases were evaluated. Clinical effects were excellent in 543 cases (29.4%) and good in 822 cases (44.6%), and the efficacy rate for cases judged as excellent and good comprised 74.0%. 4. Comparative studies in which the efficacy of ASPC was compared to efficacies of PIPC and SBPC were performed in patients with respiratory tract infections, postoperative wound infections and suppurative otitis media. ASPC showed satisfactory clinical effects in all trials. 5. In the above open and comparative clinical studies of ASPC, incidence of adverse side reaction was only 1.95% (45/2,304), and main side effects were skin rash and diarrhea.
Activity of sub-minimal inhibitory concentrations of Aspoxicillin in prolonging the postantibiotic effect against Staphylococcus aureus
J Antimicrob Chemother 1990 Jul;26(1):29-38.PMID:2211444DOI:10.1093/jac/26.1.29.
Aspoxicillin, a newly developed acylureido-penicillin with a long half-life in mouse serum of 55 min, induced postantibiotic effects (PAEs) against Staphylococcus aureus Smith of 1.7 h in vitro and 5.2 h in vivo in a thigh infection model in neutropenic mice. The long serum half-life meant that in order to evaluate the in-vivo PAE, it was necessary to examine the contribution of the drug at a sub-minimal inhibitory concentration (sub-MIC). Growth suppression by sub-MICs of Aspoxicillin was examined in vitro using either previously unexposed bacterial cells or cells which had been pre-exposed to twice the MIC of Aspoxicillin for 2 h. At each sub-MIC tested, the duration of growth suppression for pre-exposed cells was longer than that for unexposed cells. In an attempt to eliminate the sub-MIC effect in vivo, penicillinase was injected into mice at the time after administration when the Aspoxicillin serum concentration approached the MIC. The in-vivo PAE decreased to 2.7 h when penicillinase was injected. It was concluded that Aspoxicillin induced a PAE in vivo which was additional to the effect of sub-inhibitory residual drug, but that sub-MIC levels of the drug were simultaneously involved in suppressing bacterial regrowth after the drug concentration decreased below the MIC. Similar postantibiotic sub-MIC effects may also occur with other long half-life antibiotics.
Determination of Aspoxicillin (TA-058) by high-performance liquid chromatography. Stability at different temperatures
Zentralbl Bakteriol Mikrobiol Hyg A 1987 Jun;265(1-2):176-81.PMID:3673331DOI:10.1016/s0176-6724(87)80164-5.
A rapid and sensitive HPLC-method has been developed for the determination of serum concentrations of Aspoxicillin (TA-058), a new semisynthetic beta-lactam antibiotic. Aspoxicillin was chromatographed with a phosphate buffer/methanol (92:8 v/v) mobile phase and a C-18 reversed phase column and was detected at a wavelength of 220 nm. The stability of Aspoxicillin in serum and buffer at different temperatures was studied over a time period of 3 months. Furthermore, the degradation of Aspoxicillin versus piperacillin was determined in serum and buffer at 37 degrees C. Aspoxicillin remains stable only at -70 degrees C whereas degradation has been observed at -20 degrees C and 4 degrees C. At 37 degrees C, 20% of Aspoxicillin is degraded in serum within 24 h whereas piperacillin is completely degraded under the same conditions.
Effect of Aspoxicillin on anaerobic bacteria
Jpn J Antibiot 1985 Jun;38(6):1516-28.PMID:3850132doi
Aspoxicillin (ASPC), a semisynthetic penicillin has a broad spectrum of antibacterial activities against Gram-positive and Gram-negative anaerobic bacteria. Its in vitro antibacterial activity was less than those of cefoxitin against Peptostreptococcus and Veillonella, but was significantly high against Bacteroides fragilis, one of the most clinically important anaerobe. The therapeutic and/or protective effect of ASPC in experimental subcutaneous abscess or experimental intraabdominal mixed infection due to beta-lactamase producing B. fragilis and non-producing Escherichia coli were much stronger than those of ticarcillin. In order to account the superiority of ASPC in vivo, the effects of ASPC and other beta-lactams on B. fragilis were compared and the results were analyzed in relation to their in vitro bactericidal activities, stability against the beta-lactamase, binding properties with penicillin-binding proteins and pharmacokinetic properties. Interestingly, administration of ASPC did not increase the bacterial counts of Clostridium difficile in caecal contents, but piperacillin, ticalcillin, carbenicillin, ampicillin and cefotaxime increased the counts.