GGsTop
Based on 7 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.82%
- No. CAS: 926281-37-0
- Fòrmula: C13H18NO7P
- Peso molecular:331.26
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GGsTop
More- Nature. 2026 May;653(8115):933-941. [Abstract]
- ACS Nano. 2020 Apr 28;14(4):4890-4904. [Abstract]
- Small. 2020 Nov;16(44):e2004172. [Abstract]
- Mater Today Bio. 2025 Jun 13:33:101964. [Abstract]
- J Med Chem. 2026 May 28;69(10):12417-12429. [Abstract]
- Anal Chem. 2025 Jul 22;97(28):15393-15401. [Abstract]
- bioRxiv. 2024 Oct 13:2024.10.10.617667. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Actividad biológica
Descripciòn
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GGsTop also reduces 4-HNE and TNF-α production, and decreases hepatic necrosis in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats (9 week old)[3]
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Dosage:1 mg/kg
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Administration:Injected into the inferior vena cava for 12, 24, 48 h
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Result:Lowered the serum levels of ALT, AST, prevented the increase of serum γ-GT levels in IR-GGsTop group.
Chemical Information
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No. CAS 926281-37-0
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Appearance Solid
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Peso molecular 331.26
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Fòrmula C13H18NO7P
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Color White to off-white
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SMILES
O=C(O)CC1=CC=CC(OP(OC)(CCC(N)C(O)=O)=O)=C1
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Synonyms
Nahlsgen
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Nature
2026 May;653(8115):933-941. PMID: 41851454
GGsTop purchased from MedChemExpress. Usage Cited in: Nature. 2026 May;653(8115):933-941. [Abstract]
GGT activity in HCC-1806 cells treated with GGsTop for 4 h.
GGsTop purchased from MedChemExpress. Usage Cited in: Nature. 2026 May;653(8115):933-941. [Abstract]
Relative cell numbers of HCC-1806 cells treated with GGsTop (10-10000 nM) for 96 h in control or cystine-free medium supplemented with GSH or CysGly.
GGsTop purchased from MedChemExpress. Usage Cited in: Nature. 2026 May;653(8115):933-941. [Abstract]
GGT activity in kidney extracts of mice intraperitoneally (i.p.) injected with vehicle (n = 6 mice) or with 5 mg/kg of GGsTop every 12 h for 1 (n = 9), 2 (n = 9) or 3 days (n = 8).
GGsTop purchased from MedChemExpress. Usage Cited in: Nature. 2026 May;653(8115):933-941. [Abstract]
Tumour volume of orthotopic HCC-1806 xenografts in mice treated with vehicle (n = 15) or 5 mg/kg GGsTop (n = 18) every 12 h.
GGsTop purchased from MedChemExpress. Usage Cited in: Nature. 2026 May;653(8115):933-941. [Abstract]
Tumour volume of orthotopic HCC-1806 xenografts treated with vehicle or 5 mg/kg GGsTop every 12 h alone or supplemented with NAC (30 mM) in drinking water (vehicle, n = 5; GGsTop, n = 8; vehicle with NAC, n = 5, GGsTop with NAC, n = 7, representative of 2 independent experiments).
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ACS Nano
Enzyme-Triggered Transcytosis of Dendrimer-Drug Conjugate for Deep Penetration into Pancreatic Tumors. [Abstract]2020 Apr 28;14(4):4890-4904. PMID: 32286784 -
Small
Active Transportation of Liposome Enhances Tumor Accumulation, Penetration, and Therapeutic Efficacy. [Abstract]2020 Nov;16(44):e2004172. PMID: 33030305 -
Mater Today Bio
γ-glutamyl transpeptidase-catalyzed polymer-enzyme-drug conjugate enhances penetration and suppression in oral squamous cell carcinoma via transdermal application. [Abstract]2025 Jun 13:33:101964. PMID: 40605992 -
J Med Chem
Enzyme-Triggered Charge and Conformation Switching for Tumor-Selective Peptide-Drug Conjugates. [Abstract]2026 May 28;69(10):12417-12429. PMID: 42142047 -
Anal Chem
2025 Jul 22;97(28):15393-15401. PMID: 40557718 -
bioRxiv
2024 Oct 13:2024.10.10.617667. PMID: 39416022
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (301.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0188 mL | 15.0939 mL | 30.1878 mL | 75.4694 mL |
| 5 mM | 0.6038 mL | 3.0188 mL | 6.0376 mL | 15.0939 mL | |
| 10 mM | 0.3019 mL | 1.5094 mL | 3.0188 mL | 7.5469 mL | |
| 15 mM | 0.2013 mL | 1.0063 mL | 2.0125 mL | 5.0313 mL | |
| 20 mM | 0.1509 mL | 0.7547 mL | 1.5094 mL | 3.7735 mL | |
| 25 mM | 0.1208 mL | 0.6038 mL | 1.2075 mL | 3.0188 mL | |
| 30 mM | 0.1006 mL | 0.5031 mL | 1.0063 mL | 2.5156 mL | |
| 40 mM | 0.0755 mL | 0.3773 mL | 0.7547 mL | 1.8867 mL | |
| 50 mM | 0.0604 mL | 0.3019 mL | 0.6038 mL | 1.5094 mL | |
| 60 mM | 0.0503 mL | 0.2516 mL | 0.5031 mL | 1.2578 mL | |
| 80 mM | 0.0377 mL | 0.1887 mL | 0.3773 mL | 0.9434 mL | |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3019 mL | 0.7547 mL |
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