Cefetrizole
Cefetrizole Basic information
- Product Name:
- Cefetrizole
- Synonyms:
-
- 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:
- 65307-12-2
- MF:
- C16H15N5O4S3
- MW:
- 437.52
- Mol File:
- 65307-12-2.mol
Cefetrizole Chemical Properties
- Density
- 1.71±0.1 g/cm3(Predicted)
- pka
- 2.65±0.50(Predicted)
Cefetrizole Usage And Synthesis
Uses
Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.
Biological Activity
Ceftezole is an α-Glucosidase inhibitor with IC50 and Ki values of 2.1 μM and 0.578 μM, respectively.
in vitro
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.
in vivo
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].
target
IC50: 2.1 μM (α-Glucosidase)
Ki: 0.578 μM (α-Glucosidase)
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. PMID:17671744
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