APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.
APX-115 (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line.
In the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes.
体内研究
APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice.
APX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels.
Animal Model:
Six-week-old male diabetic db/db mice (C57BLKS/J-lepr/lepr)
Dosage:
60 mg/kg
Administration:
Oral gavage; per day; for 12 weeks
Result:
Significantly improved insulin resistance in diabetic mice.
分子式
C17H18ClN3O
分子量
315.80
CAS号
1395946-75-4
运输条件
Room temperature in continental US; may vary elsewhere.