| 货号 | 17764-1mg |
| 描述 | NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.1,2 GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.3 It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.3,4 GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.3,4,5 It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.6,7,8 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Chen, F.,Haigh, S.,Barman, S., et al. From form to function: The role of Nox4 in the cardiovascular system. Front.Physiol. 3, (2012). 2.Konior, A.,Schramm, A.,Czesnikiewicz-Guzik, M., et al. NADPH oxidases in vascular pathology. Antioxidants & Redox Signaling 20(17), 2794-2814 (2014). 3.Jiang, J.X.,Chen, X.,Serizawa, N., et al. Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo. Free Radical Biology & Medicine 53(2), 289-296 (2012). 4.Laleu, B.,Gaggini, F.,Orchard, M., et al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. Journal of Medicinal Chemistry 53(21), 7715-7730 (2010). 5.Aoyama, T.,Paik, Y.H.,Watanabe, S., et al. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology 56(6), 2316-2327 (2012). 6.Green, D.E.,Murphy, T.C.,Kang, B.Y., et al. The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. American Journal of Respiration, Cell, and Molecular Biology 47(5), 718-726 (2012). 7.Choi, D.H.,Kim, J.H.,Seo, J.H., et al. Matrix metalloproteinase-3 causes dopaminergic neuronal death through Nox1-regenerated oxidative stress. PLoS One 9(12), (2014). 8.Jha, J.C.,Gray, S.P.,Barit, D., et al. Genetic targeting or pharmacologic inhibition of NADPH oxidase nox4 provides renoprotection in long-term diabetic nephropathy. Journal of the American Society of Nephrology 25(6), 1237-1254 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 394.9 |
| 分子式 | C21H19ClN4O2 |
| CAS号 | 1218942-37-0 |
| 稳定性 | ≥ 2 years |
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