ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors 2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione

2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione

Product Name2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
CAS1218942-37-0
MFC21H19ClN4O2
MW394.85
EINECS942-974-8
MOL File1218942-37-0.mol

Chemical Properties

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.

Usage And Synthesis

Description

GKT-137831 (1218942-37-0) is an NADPH oxidase, NOX1/4 inhibitor (Ki= 100-150 nM).1 Inhibits erastin-stimulated ROS production.2Potentiates immunotherapy by overcoming cancer-associated fibroblast- mediated CD8+T-cell exclusion.3Reduces ROS production in LPS-stimulated platelets in a mouse model.4Reduces subarachnoid hemorrhage-induced neuronal death.5Potent 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] JOY X. JIANG . Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo[J]. Free Radical Biology and Medicine, 2012, 53 2: Pages 289-296. DOI:10.1016/j.freeradbiomed.2012.05.007
[2] JASMIN DÄCHERT. Targeting ferroptosis in rhabdomyosarcoma cells[J]. International Journal of Cancer, 2019, 146 2: 510-520. DOI:10.1002/ijc.32496
[3] KIRSTY FORD. NOX4 Inhibition Potentiates Immunotherapy by Overcoming Cancer-Associated Fibroblast-Mediated CD8 T-cell Exclusion from Tumors.[J]. Cancer research, 2020, 80 9: 1846-1860. DOI:10.1158/0008-5472.can-19-3158
[4] ANA C ANTUNES NAIME. Tumor necrosis factor alpha has a crucial role in increased reactive oxygen species production in platelets of mice injected with lipopolysaccharide.[J]. Platelets, 2019: 1047-1052. DOI:10.1080/09537104.2019.1588241
[5] LI ZHANG. Involvement of Nox2 and Nox4 NADPH oxidases in early brain injury after subarachnoid hemorrhage.[J]. Free Radical Research, 2017, 51 3: 316-328. DOI:10.1080/10715762.2017.1311015
[6] TOMONORI AOYAMA. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent†‡[J]. Hepatology, 2012, 56 6: 2316-2327. DOI:10.1002/hep.25938

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