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Product introduction
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
Chinese name
Setanaxib (GKT137831), 细胞色素 b-245 beta 链抑制剂
English name
Setanaxib (GKT137831)
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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Setanaxib (GKT137831) 10mM in DMSO 1ml

Setanaxib (GKT137831) 10mM in DMSO 1ml; supplied for laboratory research, analysis, inspection, and scientific procurement use; specifications: 1ml.

item number:S407890-1ml
Product model:1ml
level: 1ml
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