Product Name: GKT-137831
GKT-137831 Chemical Structure
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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.
IC50 value: 140±40 nM/110±30 nM(Nox1/Nox4, Ki)
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
Solubility:Soluble in DMSO
Storage Conditions: Room temperature, or -20ºC for 3 years.
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