APX-115 (C09-1102-525)

APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1 , Nox2 and Nox4 , respectively. APX-115 effectively prevents kidney injuryIn VitroAPX-115 (5?μM; 60?min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line. ?/nIn the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAPX-115 (oral gavage; 60?mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice. ?/nAPX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db )Dosage: 60 mg/kg Administration: Oral gavage; per day; for 12 weeks Result: Significantly improved insulin resistance in diabetic mice.Form:SolidIC50& Target:NOX1 NOX2 NOX4. Specification: 0.99 Molecular Formula: C17H18ClN3O Molecular Weight: 315.8 PubChem CID: 60172240 Isomeric SMILES: CCCC1=C(NN(C1=O)C2=CC=CC=N2)C3=CC=CC=C3.Cl