65307-12-2
65307-12-2 結(jié)構(gòu)式
基本信息
中文別名
頭孢三唑頭孢三唑原料
英文別名
Cefetrizole(6R,7R)-8-Oxo-7-[2-thienylacetylamino]-3-[(1H-s-triazol-3-ylthio)methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 8-oxo-7-[[2-(2-thienyl)acetyl]amino]-3-[(1H-1,2,4-triazol-5-ylthio)methyl]-, (6R,7R)-
所屬類別
醫(yī)藥中間體：原料藥中間體常見問題列表
生物活性
Ceftezole 是一種 α-Glucosidase 抑制劑，其 IC50 和 Ki 值分別為 2.1 μM 和 0.578 μM。靶點
IC50: 2.1 μM (α-Glucosidase)
Ki: 0.578 μM (α-Glucosidase)
體外研究
In in vitro α-Glucosidase assays, Ceftezole is shown to be a reversible, non-competitive inhibitor of yeast α-glucosidase with a K i value of 5.78×10 -7 M when the enzyme mixture is pretreated with ceftezole.
體內(nèi)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 (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.