GK-136901
CAS No. : 1062624-71-8
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| Cat. No. : | HY-124487 |
| M.Wt: | 346.38 |
| Formula: | C20H18N4O2 |
| Purity: | >98 % |
| Solubility: |
GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a Ki 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[1][2][3][4].
In Vitro:GKT136901 (10 μM; 30 min) inhibits NADPH oxidase activity and ROS production induced by high D-glucose in MPT cells[2].
GKT136901 (10 μM; 30 min) inhibits the expression of profibrotic proteins and the activation of p38MAP kinase in MPT cells induced by high D-glucose[2].
In Vivo:GK-136901 attenuates hypoxia-induced pulmonary vascular cell proliferation in a mouse model of pulmonary arterial hypertension[4].
GK-136901 is well tolerated in mice, with oral administration doses tested up to 1000 mg/kg[5].
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