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APX-115 free base (Ewha-18278 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。
APX-115 free base (Ewha-18278 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 413 | 现货 | |
5 mg | ¥ 997 | 现货 | |
10 mg | ¥ 1,660 | 现货 | |
25 mg | ¥ 3,490 | 现货 | |
50 mg | ¥ 5,520 | 现货 | |
100 mg | ¥ 7,730 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,190 | 现货 |
产品描述 | APX-115 free base (Ewha-18278 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. |
靶点活性 | NOX1:ki:1.08 μM , Nox4:0.63 μM (ki), NOX2:0.57 μM (ki) |
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. |
别名 | Ewha-18278 free base |
分子量 | 279.34 |
分子式 | C17H17N3O |
CAS No. | 1270084-92-8 |
Smiles | CCCc1c(O)n(nc1-c1ccccc1)-c1ccccn1 |
密度 | 1.17 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 245 mg/mL (877.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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