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 Structure](CAS/20150408/GIF/1218942-37-0.gif)
- 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
- Molecular Weight:
- 394.85
- MDL Number:
- MFCD27923122
- MOL File:
- 1218942-37-0.mol
- MSDS File:
- SDS
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione 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. |
| FDA UNII | 45II35329V |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione price More Price(23)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 5mg | $74 | 2024-03-01 | Buy |
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 10mg | $124 | 2024-03-01 | Buy |
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 25mg | $455 | 2021-12-16 | Buy |
| TRC | C376575 | 2-(2-Chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione | 1218942-37-0 | 10mg | $220 | 2021-12-16 | Buy |
2-(2-Chlorophenyl)-4-(3-(diMethylaMino)phenyl)-5-Methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione Chemical Properties,Uses,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) 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
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32299 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30230 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| Labnetwork lnc. | +86-27-50766799 +8618062016861 | contact@labnetwork.com | China | 19987 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38671 | 58 |
