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; displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice

GKT137831 – 5 mg

Brand:
Cayman
CAS:
1218942-37-0
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

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; displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice

Formal name: 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-1H-pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione

Synonyms: 

Molecular weight: 394.9

CAS: 1218942-37-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Kidney & Renal Disease|Diabetic Nephropathy||Research Area|Cardiovascular System|Vasculature||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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