Molecular Formula | C21H19ClN4O2 |
Molar Mass | 394.85 |
Density | 1.42±0.1 g/cm3(Predicted) |
Boling Point | 560.5±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 37 mg/mL |
Appearance | solid |
Color | Pale yellow |
pKa | 5.13±0.25(Predicted) |
Storage Condition | -20°C |
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. |
In vitro study | In HPAECs and HPASMCs, GKT137831 attenuated hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression, and improved PPARγ expression reduction. In human artery endothelial cells, GKT137831 also protects against oxidative stress in response to hyperglycemia. |
In vivo study | In WT and SOD1 Mut mice, GKT137831 (60 mg/kg I. g.) blocked liver fibrosis and downregulated oxidative stress, inflammation, and fibrosis. GKT137831 (60 mg/kg/d p.o.) it also attenuates long-term hypoxia-induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and changes in lung PPARγ and TGF-β expression under hypoxia. In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetic accelerated atherosclerosis. In addition, in c-hNox4Tg mice injected with Ang II, GKT137831 abolished the increase in oxidative stress, inhibited Akt-mTOR and NF-κB signaling pathways, and attenuated cardiac remodeling. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.533 ml | 12.663 ml | 25.326 ml |
5 mM | 0.507 ml | 2.533 ml | 5.065 ml |
10 mM | 0.253 ml | 1.266 ml | 2.533 ml |
5 mM | 0.051 ml | 0.253 ml | 0.507 ml |