Cefetrizole
(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。
Cas No.:65307-12-2
Sample solution is provided at 25 µL, 10mM.
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.
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. |
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 |
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。 |
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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 |
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。
Quality Control & SDS
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- Purity: >98.00%
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