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GGsTop (Synonyms: Nahlsgen)

Cat. No.: HY-108467
Handling Instructions

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.

For research use only. We do not sell to patients.

GGsTop Chemical Structure

GGsTop Chemical Structure

CAS No. : 926281-37-0

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Based on 1 publication(s) in Google Scholar

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Description

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]

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].

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].

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.
Storage

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

References
Molecular Weight

331.26

Formula

C₁₃H₁₈NO₇P

CAS No.

926281-37-0

SMILES

O=C(O)CC1=CC=CC(OP(OC)(CCC(N)C(O)=O)=O)=C1

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GGsTop
Cat. No.:
HY-108467
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GGsTop

Cat. No.: HY-108467