GGsTop (Synonyms: Nahlsgen)

GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a K_i of 170 μM for Human GGT. GGsTop shows a pK_a of 9.71, also exhibits K_ons 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].

Ki: 170 μM (Human GGT)^[1]

GGsTop (Nahlsgen; Compound 5a) is a potent, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a K_i of 170 μM for Human GGT^[1]. GGsTop shows pK_a of 9.71, also exhibits K_ons 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.

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.

331.26

C₁₃H₁₈NO₇P

926281-37-0

Room temperature in continental US; may vary elsewhere.

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

• [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.