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Cefetrizole Sale

(Synonyms: 头孢三唑) 目录号 : GC31580

Ceftezole是一种α-Glucosidase抑制剂,其IC50和Ki值分别为2.1μM和0.578μM。

Cefetrizole Chemical Structure

Cas No.:65307-12-2

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Kinase experiment:

Ceftezole at the designated concentrations is added to the enzyme buffer solution and incubated at 30˚C for 1 h, and the substrate is then added to start the enzyme reaction. When pretreatment is not specified, mixtures of substrate and Ceftezole at various concentrations are prepared beforehand and added to the enzyme solution. Enzyme reactions are performed at 30˚C for 30 min, and 3 vol of 1 M sodium carbonate are then added to stop the reaction. The total reaction volume is 100 μL. Enzymatic activity is quantified by measuring the absorbency at 405 nm[1].

Animal experiment:

Diabetes is induced by intravenous STZ injections [30 mg/kg in fresh 10 mM sodium citrate buffer (pH 4.5)] into veins of mice in one diabetic control group and one treatment group. Diabetic female mice are identified as those having blood glucose levels >250 mg/dL using a kit. Ceftezole or vehicle (distilled water) is given intraperitoneally (30 mg/kg/day) every day for 14 days. Twenty-four hours after the final Ceftezole treatment, mice are anesthetized with pure diethylether inhalation, and blood analysis is carried out[1].

References:

[1]. Lee DS, et al. 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.

产品描述

Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.

In in vitro α-Glucosidase assays, Ceftezole is 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 is pretreated with ceftezole[1].

Using an in vivo streptozotocin-induced mouse model, blood glucose levels are confirmed to be decreased by 30% 20 min after Ceftezole treatment (10 mg/kg/day). Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-γ, and uncoupling protein-3 mRNA are also slightly decreased compare to controls following Ceftezole treatment[1].

[1]. Lee DS, et al. 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.

Chemical Properties

Cas No. 65307-12-2 SDF
别名 头孢三唑
Canonical SMILES OC(C1=C(CSC2=NN=CN2)CS[C@@]([C@@H]3NC(CC4=CC=CS4)=O)([H])N1C3=O)=O
分子式 C16H15N5O4S3 分子量 437.52
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2856 mL 11.428 mL 22.8561 mL
5 mM 0.4571 mL 2.2856 mL 4.5712 mL
10 mM 0.2286 mL 1.1428 mL 2.2856 mL
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Research Update

Behaviors and physical mechanism of ceftezole sodium de-agglomeration driven by ultrasound

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.

Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity

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

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.

Pharmacokinetic studies on ceftezole

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

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.