APX-115 (Ewha-18278) 是一种有效的,口服活性的,非选择性 Nox 抑制剂,对 Nox1,Nox2 和 Nox4 的 Ki 值分别为 1.08 μM,0.57 μM 和 0.63 μM。APX-115 可有效预防糖尿病小鼠的肾损伤。
产品描述
APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor (Kis: 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2, and Nox4). APX-115 effectively prevents kidney injury.
体外活性
In the mouse podocyte cell line, APX-115 (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression. In the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes [2].
体内活性
APX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels. APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice[1].
Cas No.
1395946-75-4
分子式
C17H18ClN3O
分子量
315.8
别名
Ewha-18278
储存和溶解度
DMSO:90mg/mL (285mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years