产品
编 号:F523743
分子式:C13H18NO7P
分子量:331.26
产品类型
结构图
CAS No: 926281-37-0
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产品详情
生物活性:
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ?glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M-1 s-1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
体内研究:
GGsTop (1 mg/kg) lowers levels of ALT, AST, γ-GT at 12, 24, and 48 h after ischemia-reperfusion in rats. GGsTop also reduces 4-HNE and TNF-α production, and decreases hepatic necrosis in rats.Animal Model:Male rats (9 week old)
Dosage:1 mg/kg
Administration:Injected into the inferior vena cava for 12, 24, 48 h
Result:Lowered the serum levels of ALT, AST, prevented the increase of serum γ-GT levels in IR-GGsTop group.
体外研究:
GGsTop (Nahlsgen; Compound 5a) is a potent, highly selective and irreversible γ?glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M-1 s-1 against E.coli GGT and human GGT, respectively.GGsTop is non-toxic compound, completely inhibits WT human GGT in 1 min at 1 mM, but less potent against the K562S mutant.