Cefazedone
(Synonyms: 头孢西酮,Refosporen) 目录号 : GC39542
Cefazedone (Refosporen, Cefazedonum) is a semisynthetic first-generation cephalosporin with antibacterial activity.
Cas No.:56187-47-4
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
Cefazedone (Refosporen, Cefazedonum) is a semisynthetic first-generation cephalosporin with antibacterial activity.
Ceftezole exhibited potent α-glucosidase inhibitory activity. In in vitro α-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast α-glucosidase with a Ki value of 5.78×10?7 M when the enzyme mixture was pretreated with ceftezole[2].
In mice, dogs, and rabbits, cefazedone produced high and prolonged serum levels. It does not penetrate the CSF or brain tissue[1]. Ceftezole inhibits the blood glucose increase that occurs following glucose uptake. Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-γ, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following ceftezole treatment. It exhibits anti-diabetic activity in vivo[2].
[1] Dingeldein E, et al. Arzneimittelforschung. 1979, 29(2a):400-3. [2] Lee DS, et al. Int J Mol Med. 2007, 20(3):379-83.
| Cas No. | 56187-47-4 | SDF | |
| 别名 | 头孢西酮,Refosporen | ||
| Canonical SMILES | O=C(O)C(N1[C@@]([H])([C@@H](C1=O)NC(CN(C=C(C2=O)Cl)C=C2Cl)=O)SC3)=C3CSC4=NN=C(S4)C | ||
| 分子式 | C18H15Cl2N5O5S3 | 分子量 | 548.44 |
| 溶解度 | DMSO: 125 mg/mL (227.92 mM) | 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 | 1.8234 mL | 9.1168 mL | 18.2335 mL |
| 5 mM | 0.3647 mL | 1.8234 mL | 3.6467 mL |
| 10 mM | 0.1823 mL | 0.9117 mL | 1.8234 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。
Determination of Cefazedone in human plasma by high performance liquid chromatography-tandem mass spectrometry: Application to a pharmacokinetic study on Chinese volunteers
J Chromatogr B Analyt Technol Biomed Life Sci 2010 Oct 15;878(28):2911-5.PMID:20813593DOI:10.1016/j.jchromb.2010.08.008.
A rapid, sensitive and simple high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for determination of Cefazedone in human plasma using metronidazole as internal standard (IS). The chromatographic separation was achieved on an Ultimate XB-CN column (2.1mm×150mm, 5μm) with an isocratic mobile phase of acetonitrile and 20mM ammonium acetate in 0.1% formic acid in water (15:85, v/v). Detection was performed using electrospray ionization in positive ion multiple reaction-monitoring mode (SRM), monitoring the transitions m/z 548.2→344.1 for Cefazedone and m/z 172.2→128.1 for IS. Calibration curves were linear over a wide range of 0.20-401.12μg/mL for Cefazedone in plasma. The lower limit of quantification (LLOQ) was 0.20μg/mL. The intra- and inter-day precisions were less than 7.2%. The average recovery of Cefazedone was 90.8-91.0%. The validated method was successfully applied to the pharmacokinetic study of Cefazedone in Chinese healthy volunteers following intravenous (IV) administration of 500, 1000 and 2000mg Cefazedone injection.
A Pharmacokinetic and Pharmacodynamic Study on Intravenous Cefazedone Sodium in Patients with Community-acquired Pneumonia
Chin Med J (Engl) 2015 May 5;128(9):1160-4.PMID:25947397DOI:10.4103/0366-6999.156086.
Background: As a time-dependent antibiotic, the time of Cefazedone concentration exceeds the minimum inhibitory concentration (MIC) is the key pharmacokinetic-pharmacodynamic (PK-PD) variable associated with the killing of pathogens. The purpose of the study was to evaluate the clinical regimen rationality of intravenous Cefazedone sodium in the treatment of community-acquired pneumonia (CAP) by PK/PD study. Methods: Ten patients with mild to moderate CAP were enrolled to receive intravenous Cefazedone sodium (2 g q12 h) for 7-14 days. Blood samples were collected in any day during day 5-7. Sputum specimens were collected before treatment for bacteria isolated, and susceptibility to Cefazedone determined. PK-PD analysis was performed using the noncompartmental analysis of Phoenix WinNolin software (version 6.1, Pharsight Corporation, CA, USA). The maximal time above MIC (ƒT > MIC) was calculated, and its correlation with clinical efficacy was analyzed. Results: All 10 patients completed the study and 8 of them were cured. Six strains were isolated from patients before treatment (one for each patient) and all susceptible to Cefazedone. Five patients of six in culture positive group were cured. All pathogens were cleared at the end of therapy. The MICs were between 0.25 and 1 mg/L. The main PK parameters were C max 175.22 ± 36.28 mg/L; T½ 1.52 ± 0.23 h; AUC (0-∞) 280.51 ± 68.17 mg·L -1·h -1 ; CL 7.37 ± 1.84 L/h; Vd 16.06 ± 4.42 L. The average ƒT > MIC was 55.45 ± 8.12%. Conclusions: Intravenous injection of cefazodone sodium with 2 g q12 h dosage regimen is used in the treatment of CAP caused by sensitive bacteria, either ƒT > MIC or clinical efficacy shows that such dosing regimen is reasonable.
[The diffusion of Cefazedone into heart muscle, prostatic and skin tissue and into bile]
Arzneimittelforschung 1979;29(12):1901-6.PMID:546431doi
The diffusion of Cefazedone into human heart muscle, prostatic and skin tissue as well as bile fluid was investigated. 40 to 80 min after a single injection of 100 mg/kg (n = 14) the concentration in the heart muscle was between 10.8 and 85.5 micrograms/g. The respective serum levels were between 117 and 168.1 micrograms/ml. The single i.v. injection of 2 g Cefazedone resulted within 30 min in a mean concentration of 34.63 +/- 9.75 micrograms/g in the prostatic tissue and in serum levels of 139.07 +/- 39.68 micrograms/ml (n = 14). In 5 patients additional values were estimated after 60 min. At this time the antibiotic concentrations were 24.92 +/- 1.31 micrograms/g in the tissue, with simultaneous serum levels of 87.25 +/- 20.86 micrograms/ml. 1 h after a 500 mg i.v. dose, concentrations in bile taken from T-tube were between 71.4 and 210 micrograms/ml. After 2 h there was a mean level of 83.2 micrograms/ml which was significantly above the serum concentrations at the same time (1 h = 35.25 +/- 7.17; and 2 h = 20.5 micrograms/ml). The bile concentration of 2 patients taken 5 h after Cefazedone injection was 4.95 and 11.6 micrograms/ml. The Cefazedone concentrations in the skin were estimated mainly in biopsies from granulating leg ulcer tissues. The mean concentrations in 4 cases were 120 +/- 28.7 micrograms/g 3 h after i.v. injection of 2 g Cefazedone. The simultaneous serum levels were between 14.85 and 68.2 micrograms/ml, in one patient with extreme venous stasis the tissue concentration was only 8.1 micrograms/g. Cefazedone should be regarded as an antibiotic with excellent penetration into tissues.
The hematologic effects of cefonicid and Cefazedone in the dog: a potential model of cephalosporin hematotoxicity in man
Toxicol Appl Pharmacol 1987 Aug;90(1):135-42.PMID:3629586DOI:10.1016/0041-008x(87)90314-0.
Cephalosporin antibiotics cause a variety of hematologic disturbances in man, the pathogeneses and hematopathology of which remain poorly characterized. There is a need for a well-defined animal model in which these blood dyscrasias can be studied. In four subacute toxicity studies, the intravenous administration of cefonicid or Cefazedone to beagle dogs caused a dose-dependent incidence of anemia, neutropenia, and thrombocytopenia after 1-3 months of treatment. A nonregenerative anemia was the most compromising of the cytopenias and occurred in approximately 50% of dogs receiving 400-500 mg/kg cefonicid or 540-840 mg/kg Cefazedone. All three cytopenias were completely reversible following cessation of treatment; the time required for recovery of the erythron (approximately 1 month) was considerably longer than that of the granulocytes and platelets (hours to a few days). Upon rechallenge with either cephalosporin, the hematologic syndrome was reproduced in most dogs tested; cefonicid (but not Cefazedone)-treated dogs showed a substantially reduced induction period (15 +/- 5 days) compared to that of the first exposure to the drug (61 +/- 24 days). This observation, along with the rapid rate of decline in red cell mass parameters of affected dogs, suggests that a hemolytic component complicated the red cell production problem and that multiple toxicologic mechanisms contributed to the cytopenia. We conclude that the administration of high doses of cefonicid or Cefazedone to dogs can induce hematotoxicity similar to the cephalosporin-induced blood dyscrasias described in man and thus provides a useful model for studying the mechanisms of these disorders.
Investigations on the effectiveness of Cefazedone in experimental E. coli pyelonephritis
Arzneimittelforschung 1979;29(2a):414-6.PMID:385009doi
The therapeutic effectiveness of (6R,7R)-7-(2-[3,5-dichloro-4-oxo-1(4H)-pyridyl]-acetamido)-3-([(5-methyl-1,3,4-thiadiazol-2-yl)-thio]methyl)-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (Cefazedone, Refosporen), cephazolin, cephacetrile and cephalothin was compared in the test model of estradiol-induced E. coli pyelonephritis in the rat. Cefazedone and cephazolin were similar in effect. The relations between results of treatment and microbiological and pharmacokinetic characteristics of the cephalosporins tested are discussed.