APX-115 free base 是口服具有活性的、非选择性的Nox抑制剂,对Nox1,Nox2和Nox4的Ki分别为 1.08 μM,0.57 μM 和 0.63 μM。它能够有效预防糖尿病小鼠的肾损伤。
产品描述
APX-115 free base (Ewha-18278 free base) 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 free base (5?μM; 60?min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression. In the kidney, APX-115 free base attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes [2].
体内活性
APX-115 free base 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.
Cas No.
1270084-92-8
分子式
C17H17N3O
分子量
279.34
别名
Ewha-18278 free base
储存和溶解度
DMSO:245mg/ml (877.07 Mm),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years