| Identification | Back Directory | [Name]
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione | [CAS]
1218942-37-0 | [Synonyms]
CS-1795
GKT-831
Setanaxib
GKT137831
GSK-137831
GKT137831, >=98%
Setanaxib GKT137831
GKT137831(Setanaxib)
GKT-137831;GKT 137831
2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6-dione
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
1H-Pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione, 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-
2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1,2-dihydro-5H-pyrazolo[4,3-c]pyridine-3,6-dione
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione GKT137831 | [EINECS(EC#)]
942-974-8 | [Molecular Formula]
C21H19ClN4O2 | [MDL Number]
MFCD27923122 | [MOL File]
1218942-37-0.mol | [Molecular Weight]
394.85 |
| Chemical Properties | Back Directory | [Boiling point ]
560.5±60.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 65 mg/ml). | [form ]
solid | [pka]
5.13±0.25(Predicted) | [color ]
Pale yellow | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
GKT-137831 (1218942-37-0) is an NADPH oxidase, NOX1/4 inhibitor (Ki?= 100-150 nM).1? Inhibits erastin-stimulated ROS production.2?Potentiates immunotherapy by overcoming cancer-associated fibroblast- mediated CD8+?T-cell exclusion.3?Reduces ROS production in LPS-stimulated platelets in a mouse model.4?Reduces subarachnoid hemorrhage-induced neuronal death.5?Potent inhibitor of experimental liver fibrosis in mouse models.6 | [Uses]
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione is a potential drug candidate, which is used in the preparation of pyrazolopyridine derivative as NADPH oxidase inhibitors. | [in vivo]
During the last half of CCl4 injections, some mice are treated with Setanaxib (GKT137831) daily. CCl4-induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor[1]. | [IC 50]
NOX1; NOX4 | [References]
1) Jiang?et al.?(2012),?Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo; Free Radic. Biol. Med.,?53?289
2) Dachert?et al.?(2020),?Targeting ferroptosis in rhabdomyosarcoma cells; Int. J. Cancer,?146(2)?510
3) Ford?et al.?(2020),?NOX4 Inhibition Potentiates Immunotherapy by Overcoming Cancer-Associated Fibroblast-Mediated CD8 T-cell Exclusion from Tumors; Cancer Res.,?80?1846
4) Naime?et al.?(2019),?Tumor necrosis factor alpha has a crucial role in increased reactive oxygen species production in platelets of mice injected with lipopolysaccharide; Platelets,?30?1047
5) Zhang?et al.?(2017),?Involvement of Nox2 and Nox4 NADPH oxidases in early brain injury after subarachnoid hemorrhage; Free Radic. Res.,?51?316
6) Aoyama?et al.?(2012),?Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent;?Hepatology,?56?2316 |
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