| References: |
GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.
in vitro: GKT137831 attenuated hypoxia-induced H(2)O(2) release, proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs in vitro. GKT137831 prevented oxidative stress in response to hyperglycemia in human aortic endothelial cells.
in vivo: The NOX1/4 inhibitor, GKT137831, attenuated liver fibrosis and ROS production in both SOD1mu and WT mice as well as messenger RNA expression of fibrotic and NOX genes. Treatment with GKT137831 suppressed ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT HSCs . GKT137831 inhibited hypoxia-induced increases in TGF-β1 and reductions in PPARγ expression and attenuated RVH and pulmonary artery wall thickness but not increases in RVSP or muscularization of small arterioles. For the detailed information of GKT137831, the solubility of GKT137831 in water, the solubility of GKT137831 in DMSO, the solubility of GKT137831 in PBS buffer, the animal experiment (test) of GKT137831, the cell expriment (test) of GKT137831, the in vivo, in vitro and clinical trial test of GKT137831, the EC50, IC50,and affinity,of GKT137831, For the detailed information of GKT137831, the solubility of GKT137831 in water, the solubility of GKT137831 in DMSO, the solubility of GKT137831 in PBS buffer, the animal experiment (test) of GKT137831, the cell expriment (test) of GKT137831, the in vivo, in vitro and clinical trial test of GKT137831, the EC50, IC50,and affinity,of GKT137831, Please contact DC Chemicals. |
