GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a K i of 160 nM for Nox1 and 165 nM for Nox4 . GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin ( fibronectin ) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension.
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