头孢三唑

中文名称:

头孢三唑

中文同义词:

头孢三唑;头孢三唑原料

英文名称:

Cefetrizole

英文同义词:

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)-

CAS号:

65307-12-2

分子式:

C16H15N5O4S3

分子量:

437.52

EINECS号:

相关类别:

Mol文件:

65307-12-2.mol

密度 

1.71±0.1 g/cm3(Predicted)

酸度系数(pKa)

2.65±0.50(Predicted)

生物活性

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

靶点

IC50: 2.1 μM (α-Glucosidase) Ki: 0.578 μM (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 K i 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 (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.