Information Setanaxib (GKT137831) Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis . Targets Ferroptosis ; NOX1 (Cell-based assay); NOX4 (Cell-based assay) ; 110 nM(Ki); 140 nM(Ki) In vitro GKT137831 attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells. In vivo In WT and SOD1mut mice, GKT137831 (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. GKT137831 (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. Moreover, in angII-infused c-hNox4Tg mice, GKT137831 abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signaling pathway and attenuates cardiac remodeling. Cell Research(from reference) Cell lines：Hypoxic HPASMC and HPAECs Concentrations：20 μM Incubation Time：72 hours
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Setanaxib (GKT137831)
Dangerous GoodsCAS number：1218942-37-0 molecular formula：C21H19ClN4O2
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | DTXSID30153432 | SCHEMBL1302603 | 1H-Pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione, 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl- | A14433 | NCGC00378460-05 | NCGC00087752-03 | SB19230 | UNII-45II35329V | AS-74753 | 2-(2-chlorophenyl)-4-[3-(dimethyl | ||
| CAS number | 1218942-37-0 | molecular formula | C21H19ClN4O2 |
| molecular weight | 394.85 g/mol | Exact mass | - |
| PSA | 55.900 Ų | logp | 2.366 |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害 H312: 皮肤接触有害 H332: 吸入有害 H302+H312+H332: 吞咽，皮肤接触或吸入有害。
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用
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