GGsTop

GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M-1 s-1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model[1][2][3].

Product Specifications

CAS Number

[926281-37-0]

Product Name Alternative

Nahlsgen

UNSPSC

12352005

Target

γ-Glutamyl Transferase (GGT)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GGsTop.html

Purity

99.35

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C13H18NO7P

Molecular Weight

331.26

References & Citations

[1]Han L, et al. Design, synthesis, and evaluation of gamma-phosphono diester analogues of glutamate as highly potent inhibitors and active site probes of gamma-glutamyl transpeptidase. Biochemistry. 2007 Feb 6;46 (5) :1432-47.|[2]Kamiyama A, et al. Phosphonate-based irreversible inhibitors of human γ-glutamyl transpeptidase (GGT) . GGsTop is a non-toxic and highly selective inhibitor with critical electrostatic interaction with an active-site residue Lys562 for enhanced inhibitory activity. Bioorg Med Chem. 2016 Nov 1;24 (21) :5340-5352.|[3]Tamura K, et al. GGsTop, a novel and specific γ-glutamyl transpeptidase inhibitor, protects hepatic ischemia-reperfusion injury in rats. Am J Physiol Gastrointest Liver Physiol. 2016 Aug 1;311 (2) :G305-12.