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GGsTop (Synonyms: Nahlsgen)

目录号: HY-108467
产品使用指南

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。

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GGsTop Chemical Structure

GGsTop Chemical Structure

CAS No. : 926281-37-0

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5 mg ¥5000
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10 mg ¥8500
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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[1][2]. GGsTop protects hepatic ischemia-reperfusion injury in rat model[3].

IC50 & Target

Ki: 170 μM (Human GGT)[1]

体外研究
(In Vitro)

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[1]. 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[1][2].
GGsTop is non-toxic compound, completely inhibits WT human GGT in 1 min at 1 mM, but less potent against the K562S mutant[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GGsTop (1 mg/kg) lowers levels of ALT, AST, γ-GT at 12, 24, and 48 h after ischemia-reperfusion in rats[3].
GGsTop also reduces 4-HNE and TNF-α production, and decreases hepatic necrosis in rats[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats (9 week old)[3]
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.
分子量

331.26

Formula

C13H18NO7P

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • 摩尔计算器

  • 稀释计算器

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