ChemicalBook > CAS DataBase List > 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 Name
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
CAS No.
1218942-37-0
Chemical 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-831;GKT137831;Setanaxib;GSK-137831;GKT137831, >=98%;Setanaxib GKT137831;GKT137831(Setanaxib);GKT-137831;GKT 137831;Setanaxib, 10 mM in DMSO
CBNumber
CB62672829
Molecular Formula
C21H19ClN4O2
Formula Weight
394.85
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 Property

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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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17764
Product name
GKT137831
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
17764
Product name
GKT137831
Purity
≥95%
Packaging
5mg
Price
$74
Updated
2024/03/01
Cayman Chemical
Product number
17764
Product name
GKT137831
Purity
≥95%
Packaging
10mg
Price
$124
Updated
2024/03/01
Cayman Chemical
Product number
17764
Product name
GKT137831
Purity
≥95%
Packaging
25mg
Price
$455
Updated
2021/12/16
TRC
Product number
C376575
Product name
2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
Packaging
10mg
Price
$220
Updated
2021/12/16
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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,Usage,Production

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)-dione Preparation Products And Raw materials

Raw materials

Preparation Products

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

China 132 India 2 United States 14 Global 148
Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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China
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Chembest Research Laboratories Limited
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+86-21-20908456
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021-58180499
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sales@BioChemBest.com
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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Shanghai Macklin Biochemical Co.,Ltd.
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15221275939
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021-50706099
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shenlinxing@macklin.cn
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China
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15873
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AdooQ Bioscience CHINA
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025-58849295 18951903616;
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025-68650336
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Cool Pharm, Ltd
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021-60455363 18019463053
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50966098
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sales@coolpharm.com
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LETOPHARM LIMITED
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+86-21-5821 5861
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+86-21-5106 2861
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sales@letopharm.com
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
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+86-21-52996696
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1218942-37-0, 2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dioneRelated Search:

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  • 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%
  • 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-dione
  • GSK-137831
  • Setanaxib
  • 1H-Pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione, 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-
  • GKT-831
  • GKT137831(Setanaxib)
  • 2- ( 2 - chlorophenyl ) -4- ( 3- ( dimethylamino ) phenyl ) -5 - methyl - 1,2 - dihydro - 3H - pyrazolo [ 4 ,
  • Setanaxib, 10 mM in DMSO
  • 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1,2-dihydro-3h-pyrazolo[4,3-c]pyridine-3,6(5h)-dione
  • 1218942-37-0
  • Inhibitors
  • API