产品描述:
APX-115 is an inhibitor of NADPH oxidase 1 (NOX1), NOX2, and NOX4 (Kis = 1.08, 0.57, and 0.63 µM, respectively, for the human enzymes).{49865} It is selective for these enzymes over xanthine oxidase and glucose oxidase (Kis = >100 µM for both). APX-115 (10 or 20 µM) prevents RANKL-induced increases in reactive oxygen species (ROS) levels in primary mouse bone marrow-derived macrophages (BMDMs). It inhibits GM-CSF- and RANKL-induced primary mouse osteoclast differentiation when used at concentrations of 1.1, 3.3, or 10 µM. APX-115 (10 mg/kg per day) increases femur bone mass density and strength and reduces femur and tibia resorption areas in ovariectomized (OVX) mice. It reduces plasma and urinary levels of 8-isoprostane, a marker for lipid oxidation, plasma levels of insulin, triglycerides, HDL, LDL, and creatinine, urinary levels of albumin, as well as renal fibrosis, in a db/db mouse model of diabetic nephropathy when administered at a dose of 60 mg/kg per day.{49866}