GLX351322 acts as an inhibitor of NADPH oxidase 4, effectively reducing hydrogen peroxide production in NOX4-overexpressing cells with an IC50 value of 5 μM. It exhibits limited efficacy against NOX2 in hPBMC cells, with an IC50 of 40 μM[1].
GLX351322 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Fibroblast-like synoviocytes
20 µM
1 hour
To analyze the effect of NOX4 inhibition on cell migration induced by cytokines.
Arthritis Res Ther. 2020 May 15;22(1):116.
Primary cortical neurons
10 µM
2 hours
GLX351322 increased cell viability in Aβ1–42-treated neurons
Mol Ther. 2021 Jan 6;29(1):396-408.
Primary cortical neurons
10 µM
24 hours
GLX351322 increased the cell viability in Aβ1–42-treated neurons
Mol Ther. 2021 Jan 6;29(1):396-408.
BCPAP cells
5 µM
48 hours
GLX351322 significantly reduced cell viability under starvation independent of lenvatinib, suggesting its mechanism is different from Lenvatinib.
Cell Death Discov. 2022 Apr 8;8(1):177.
TPC-1 cells
5 µM
48 hours
GLX351322 significantly reduced cell viability under starvation independent of lenvatinib, suggesting its mechanism is different from Lenvatinib.
Cell Death Discov. 2022 Apr 8;8(1):177.
LRBCs
5 µM
48 hours
GLX351322 significantly decreased the survival ratios in lenvatinib-treated LRBCs cells independent of starvation, indicating that the combinatory usage of lenvatinib and GLX351322 can maximize the inhibitory effect.
Cell Death Discov. 2022 Apr 8;8(1):177.
GLX351322 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57Bl/6J mice
Intracranial xenograft model
Oral
3.8 mg/day/kg
Once daily for 2 weeks
GLX351322 inhibited NOX4 expression, reduced ROS production and angiogenesis, and suppressed tumor growth.
Front Pharmacol. 2022 Oct 7;13:1001588
Mice
APPswe/PS1dE9 (APP/PS1) transgenic mice
Intraperitoneal injection
5 mg/kg/day
Once daily for 4 weeks
GLX351322 treatment ameliorated synaptic and memory functions, reduced oxidative stress and amyloid levels in APP/PS1 mice
Mol Ther. 2021 Jan 6;29(1):396-408.
Mice
APP/PS1 transgenic mice
Intraperitoneal injection
5 mg/kg/day
Once daily for 4 weeks
GLX351322 improved synaptic and memory functions, and reduced oxidative stress and amyloid levels in APP/PS1 mice
Mol Ther. 2021 Jan 6;29(1):396-408.
NOD/SCID mice
BCPAP cells or LRBCs cells xenograft model
Oral
GLX351322 (5 mg/kg), Lenvatinib (30 mg/kg)
Once every 3 days for 70 days
The combination of GLX351322 and Lenvatinib completely suppressed the growth of BCPAP and LRBCs-derived tumors, significantly improving the survival rate of mice.
Cell Death Discov. 2022 Apr 8;8(1):177.
GLX351322 动物研究
Animal study
Administered orally at a dose of 3.8 mg/kg/day, GLX351322 mitigates high-fat diet-induced hyperglycemia in mice[2].
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