Ceftezole
(Synonyms: Celoslin, Falomesin) 目录号 : GC25210Ceftezole (Celoslin, Falomesin) is a semi-synthetic first-generation cephalosporin with antibacterial activity.
Cas No.:26973-24-0
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
Ceftezole (Celoslin, Falomesin) is a semi-synthetic first-generation cephalosporin with antibacterial activity.
| Cas No. | 26973-24-0 | SDF | Download SDF |
| 别名 | Celoslin, Falomesin | ||
| 分子式 | C13H12N8O4S3 | 分子量 | 440.48 |
| 溶解度 | DMSO: 88 mg/mL (199.78 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 | 2.2703 mL | 11.3513 mL | 22.7025 mL |
| 5 mM | 0.4541 mL | 2.2703 mL | 4.5405 mL |
| 10 mM | 0.227 mL | 1.1351 mL | 2.2703 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。
Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity
Int J Mol Med 2007 Sep;20(3):379-83.PMID:17671744doi
Using a high throughput-compatible assay to screen for potential alpha-glucosidase inhibitors, we found that the beta-lactam antibiotic Ceftezole exhibited potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, Ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with Ceftezole. Using an in vivo streptozotocin-induced mouse model, we confirmed that blood glucose levels decreased by 30% 20 min after Ceftezole treatment (10 mg/kg/day). Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-gamma, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following Ceftezole treatment. Taken together, these in vivo and in vitro results suggest that Ceftezole may be a clinically useful anti-diabetic compound.
Ceftezole, a new cephalosporin C derivative II. Distribution and excretion in parenteral administration
J Antibiot (Tokyo) 1976 Oct;29(10):1071-82.PMID:994326DOI:10.7164/antibiotics.29.1071.
The distribution of Ceftezole in blood and tissues and its excretion after intramuscular or intravenous administration of single doses of 10 and 20 mg/kg were compared with those of cefazolin, cephaloridine and cephalothin. Blood levels of Ceftezole in rats and rabbits were lower than those of cefazolin, and higher than those of cephaloridine and cephalothin. Retention time of Ceftezole in the blood was somewhat shorter than that of cefazolin. However, blood levels of Ceftezole in dogs were nearly the same as those of cefazolin and cephaloridine. The rate of urinary excretion of Ceftezole in 24-hour urine after administration in rats and rabbits was found to be higher than those of the other antibiotics tested. In dogs, however, the rate of urinary excretion of Ceftezole was nearly the same as that of cefazolin and higher than those of cephaloridine and cephalothin. The biliary excretion of Ceftezole in rats and dogs was much higher than those of cephaloridine and cephalothin, but lower than that of cefazolin. Tissue distribution of Ceftezole in rats was compared with that of the other antibiotics by intramuscular and intravenous administration. The initial level of Ceftezole in the kidneys was found to be substantially higher than those of the other antibiotics. The initial level of Ceftezole in the liver and lungs was also slightly higher than those of the other drugs when administered intramuscularly. Tissue levels of Ceftezole were somewhat lower than those of cefazolin in rabbits after intravenous administration. Ceftezole attained a higher maximum level in rat lymph by intramuscular administration than the other antibiotics tested. The maximum concentration of Ceftezole present in the exudate in the rat inflammatory pouch was higher than that of cefazolin. In rabbits with cerebrospinal meningitis induced by infection of Streptococcus pyogenes, the level of Ceftezole in the cerebrospinal fluid was several times higher than that in normal rabbits. The serum level and urinary excretion of Ceftezole was examined in 6 healthy male volunteers after intramuscular administration of a single dose of 500 mg. Ceftezole attained a mean maximum serum level of 22.9 mug/ml 30 minutes after administration and disappeared from the blood in about 6 hours. It was excreted rapidly in the urine. The concentration in 1-hour urine was the highest (mean level: 2,667 mug/ml) and the total excretion rate was 92.6%. No metabolites with antimicrobial activity were observed in the urine. No changes in the pattern of plasma level and urinary excretion and no accumulation in the tissues were observed after repeated intramuscular administration of 20 mg/kg of Ceftezole in rabbits, 26 times, for 14 days.
Behaviors and physical mechanism of Ceftezole sodium de-agglomeration driven by ultrasound
Ultrason Sonochem 2021 Jun;74:105570.PMID:33930689DOI:10.1016/j.ultsonch.2021.105570.
Ultrasound-mediated method, which can effectively disperse agglomerates or even eliminate agglomeration, has received more and more attentions in industrial crystallization. However, the ultrasound-mediated de-agglomeration mechanism has not been well understood, and no general conclusions have been drawn. In this study, the crystallization and de-agglomeration process of Ceftezole sodium agglomerates under ultrasound irradiation were systematically investigated. Kapur function was selected to investigate the de-agglomeration process under different ultrasonic powers. The results revealed that ultrasound could efficiently inhibit agglomeration. Besides, the de-agglomeration of large sized agglomerate particles was found to be easier to occur in comparison with small sized particles due to its higher specific breakage rate. Finally, the de-agglomeration mechanism under ultrasonic irradiation was proposed on the basis of the calculated cumulative breakage functions.
Pharmacokinetic studies on Ceftezole
Chemioterapia 1986 Dec;5(6):388-90.PMID:3802300doi
The adult volunteers were given 1 g of Ceftezole as a single intramuscular dose to investigate the pharmacokinetic profile of this new cephalosporin. The peak average serum concentration, reached 2 h after injection, was 22.5 micrograms/ml, and the t1/2 beta was 1.5 h; urinary recovery was over 80% within 24 h, the majority of injected Ceftezole being excreted within 3 hours.
In vitro and in vivo evaluation of Ceftezole, a new cephalosporin derivative
Antimicrob Agents Chemother 1976 Jul;10(1):1-13.PMID:825020DOI:10.1128/AAC.10.1.1.
Ceftezole, a new cephalosporin derivative, was compared with cefazolin, cephaloridine, and cephalothin. Data obtained indicate that it is a broad-spectrum antibiotic, with almost identical antimicrobial activity against pathogenic organisms isolated from patients. The therapeutic effect of Ceftezole on experimental infections in mice was similar to that of cefazolin and was superior to that of cephalothin. The binding of Ceftezole to serum proteins was somewhat less than that of cefazolin. The concentrations of Ceftezole in the sera of test animals and human volunteers were determined after intramuscular injection of 20 mg/kg and after a single dose of 500 mg, respectively. The concentration of Ceftezole in the serum of volunteers peaked at 24.9 mug/ml 15 min after injection and remained effective (about 2.6 mug/ml) at 4 h. The half-life in serum under the same conditions was 56 min, i.e., about one-half that of cefazolin. The 24-h urinary recovery rate was 87.5%. Most of the administered Ceftezole was excreted unchanged mainly through the urinary tract. The biliary excretion rate in SD strain rats after intramuscular injection of 20 mg/kg was about 4.4%. As compared with commercially available cephalosporins, Ceftezole was second only to cefazolin in biliary excretion rate. Various tissue levels of Ceftezole in animals were higher than cephalothin but, with the exception of renal levels in the early stage after administration, were lower than cefazolin.