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Chemical Structure| 926281-37-0 Chemical Structure| 926281-37-0

Structure of GGsTop
CAS No.: 926281-37-0

Chemical Structure| 926281-37-0

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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.

Synonyms: Nahlsgen

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Product Details of GGsTop

CAS No. :926281-37-0
Formula : C13H18NO7P
M.W : 331.26
SMILES Code : O=C(O)C(N)CCP(OC)(OC1=CC=CC(CC(O)=O)=C1)=O
Synonyms :
Nahlsgen
MDL No. :MFCD11973895

Safety of GGsTop

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow cells 50 µM 4 days To investigate the effect of GGsTop on the G-CSF-enhanced immunosuppressive function of MDSCs. GGsTop inhibited the G-CSF-enhanced immunosuppressive function of MDSCs without affecting their proliferative capacity. Front Pharmacol. 2022 Apr 25;13:873792
human periodontal ligament cells (hPLCs) 10, 20 µM 72 hours To evaluate the effect of GGsTOP on COL-I and α-SMA expression in hPLCs, results showed that GGsTOP significantly increased COL-I and α-SMA expression. Mol Med Rep. 2016 May;13(5):3813-20
human periodontal ligament cells (hPLCs) 10 µM 48 hours To evaluate the effect of GGsTOP on hPLCs migration, results showed that GGsTOP significantly promoted cell migration. Mol Med Rep. 2016 May;13(5):3813-20
human periodontal ligament cells (hPLCs) 10 µM 120 minutes To evaluate the effect of GGsTOP on ROS levels in hPLCs, results showed that GGsTOP significantly increased ROS levels. Mol Med Rep. 2016 May;13(5):3813-20
human periodontal ligament cells (hPLCs) 5, 10, 20, 50 µM 1, 3, 5, 7 days To evaluate the effect of GGsTOP on hPLCs proliferation, results showed that 10 µM GGsTOP significantly promoted cell proliferation after 7 days. Mol Med Rep. 2016 May;13(5):3813-20
human periodontal ligament cells (hPLCs) 10 µM 2 hours To evaluate the effect of GGsTOP on GGT activity in hPLCs, results showed that GGsTOP significantly inhibited GGT activity. Mol Med Rep. 2016 May;13(5):3813-20

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice 6-Hz induced seizure model and Kcna1−/− mouse model Oral gavage 13.3 mg/kg Every 12 hours for 3 days GGsTop inhibits gamma-glutamyltranspeptidase activity and promotes seizure protection Cell. 2018 Jun 14;173(7):1728-1741. e13
BALB/c male mice LPS and OVA-induced asthma exacerbation model Intratracheal administration 0.5mg/kg Once daily for 3 days GGsTop significantly attenuated hallmark features of the disease with a murine model of LPS and OVA driven asthma exacerbation, including airway hyperresponsiveness, mucus hypersecretion, collagen deposition, and expression of inflammatory cytokines. Additionally, GGsTop restored the level of glutathione, and through RNA-sequencing and pathway analysis, it was demonstrated that GGsTop downregulated the activation of the LPS/NFkB signaling pathway in the airway. Front Immunol. 2023 Jun 12;14:1132939
C57BL/6J mice EL4 lymphoma-bearing neutropenic mouse model Intraperitoneal injection 5 mg/kg Six consecutive days To evaluate the inhibitory effect of GGsTop on tumor growth during G-CSF treatment for neutropenia. GGsTop eliminated the tumor-promoting effect of G-CSF without affecting the myelopoiesis-promoting effect of G-CSF. Front Pharmacol. 2022 Apr 25;13:873792
BALB/c nude mice Xenograft model Intraperitoneal injection 1 mg/kg Every two days for a total of five times To evaluate the effect of GGsTop on tumor growth and chemosensitivity Aging (Albany NY). 2020 Jul 8;12(13):13220-13233
Wistar rats 5-FU-induced oral mucositis model Topical application to oral ulcer 1.0 μmol Once daily until ulcer healing GGsTop? shortened the treatment period for oral mucositis, promoted collagen production, and alleviated oxidative stress conditions. In Vivo. 2021 Jan-Feb;35(1):175-180
C57BL/6 mice IL-13-driven model of allergic asthma Intratracheal delivery 0.5 mg/kg Every 24 hours for three consecutive days GGsTop inhibits LLF GGT activity, increases LLF glutathione content, and attenuates IL-13-induced airway hyperreactivity and mucous production Front Pharmacol. 2014 Jul 31;5:179

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.19mL

6.04mL

3.02mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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