GGsTop

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GGsTop (Nahlsgen) 是一种有效、无毒、高度选择性和不可逆的 γ 谷酰基转肽酶 (γ?glutamyl transpeptidase (GGT)) 抑制剂，对人 GGT 的Ki 值为 170 μM。GGsTop 的 pKa 值为 9.71，对 E.coli GGT 和人 GGT 的 Kon 值分别为 150±10 和 51±3 M-1 s-1。在大鼠缺血再灌注损伤模型中，GGsTop 具有保护肝脏功能。

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.

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.

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.

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Metabolic Enzyme/Protease

Transferase

Transferase

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926281-37-0

331.26

C13H18NO7P

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (301.88 mM; 超声助溶 )

O=C(O)CC=1C=CC=C(OP(=O)(OC)CCC(N)C(=O)O)C1

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(-20℃)

With Ice Pack

≥ 2 years