Cefetrizole  

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包装规格:1mg in glass bottle
产品描述:基本信息 产品编号: C11216 产品名称: Cefetrizole CAS: 65307-12-2   储存条件 粉末 -20℃ 四年     分子式: C16H15N5O4S3 溶于液体     分子量 437.52     化学名:  (6R,7R)-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-3-(1H-1,2,4-triazol-5-ylsulfanylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid   生物活性 产品描述 一种α-Glucosidase抑制剂 靶点 IC50: 2.1μM (α-Glucosidase) Ki: 0.578μM (α-Glucosidase) 体外研究 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 体内研究 Using an in vivo streptozotocin-induced mouse model, blood glucose levels are confirmed to be decreased by 30% 20 min after Ceftezole treatment (10mg/kg/day). Expression levels of glycogen synthase kinase-3, peroxisome proliferatoractivated receptor-γ, and uncoupling protein-3 mRNA are also slightly decreased compare to controls following Ceftezole treatment   推荐实验方法(仅供参考) Kinase Assay 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 100μL. Enzymatic activity is quantified by measuring the absorbency at 405nm     Animal Administration Diabetes is induced by intravenous STZ injections [30mg/kg in fresh 10mM 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 >250mg/dL using a kit. Ceftezole or vehicle (distilled water) is given intraperitoneally (30mg/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
保存条件:-20℃