GKT137831

GKT137831

CAT N°: 17764
Price:

From 48.00 40.80

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.{28976,28981} 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.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione
  • Correlated keywords
    • 1391931-06-8 biochemical inhibitor oxidative injury apoptosis vascular disease cancer diabetes atherosclerosis cardiology hypertension GKT-137831 dual inhibit NOX1 NOX4 NOX1/NOX4 NOX-1 NOX-4 NADPH oxidase ferroptosis
  • Product Overview:
    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.{28976,28981} 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.{28980} It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.{28980,28982} GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.{28980,28982,28975} It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.{28978,28977,28979}

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