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
- Setanaxib;GKT137831;CS-1795;GKT-831;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
- TDS File:
- TDS
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(64)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 1mg | $36 | 2026-04-30 | Buy |
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 5mg | $82 | 2026-04-30 | Buy |
| Cayman Chemical | 17764 | GKT137831 ≥95% | 1218942-37-0 | 10mg | $137 | 2026-04-30 | Buy |
| Biosynth | FG137680 | GKT-137831 | 1218942-37-0 | 50mg | $272.5 | 2026-06-04 | Buy |
| Biosynth | FG137680 | GKT-137831 | 1218942-37-0 | 100mg | $500 | 2026-06-04 | 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.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
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 | |
|---|---|---|---|---|---|
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 5996 | 61 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Dalian Meilun Biotech Co., Ltd. | 0411-62910999 13889544652 | sales@meilune.com | China | 4765 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2774 | 58 |
| Shanghai Macklin Biochemical Co.,Ltd. | 15221275939 15221275939 | shenlinxing@macklin.cn | China | 15775 | 55 |
| AdooQ Bioscience CHINA | 025-58849295 | info@adooq.cn | China | 2981 | 60 |
| LETOPHARM LIMITED | +86-21-5821 5861 | sales@letopharm.com | China | 2374 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4860 | 55 |
