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

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

Product Name:
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
Synonyms:
  • CS-1795
  • GKT-137831;GKT 137831
  • Setanaxib GKT137831
  • 2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
  • GKT137831
  • 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
  • GKT137831, >=98%
CAS:
1218942-37-0
MF:
C21H19ClN4O2
MW:
394.85
EINECS:
942-974-8
Product Categories:
  • Inhibitors
  • API
Mol File:
1218942-37-0.mol
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2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione 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.
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2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione 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.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] 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

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

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
Chembest Research Laboratories Limited
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+86-21-20908456
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione(1218942-37-0)Related Product Information