| Bioactivity | APX-115 free base (Ewha-18278 free base) 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 free base effectively prevents kidney injury[1]. | ||||||||||||
| Invitro | APX-115 free base (5 μM; 60 min) 几乎完全抑制了高糖诱导的小鼠足细胞细胞系中的促炎和纤维化分子的表达[2]。在肾脏中，APX-115 free base 可减轻 Nox 基因上调和蛋白质表达，同时改善炎症和纤维化过程[2]。 | ||||||||||||
| In Vivo | APX-115 free base (口服灌胃；60 mg/kg/天；连续 12 周)可显着改善糖尿病小鼠的胰岛素抵抗[2]。APX-115 free base 治疗可降低尿蛋白排泄和血浆肌酐水平[2]。 Animal Model: | ||||||||||||
| Name | APX-115 free base | ||||||||||||
| CAS | 1270084-92-8 | ||||||||||||
| Formula | C17H17N3O | ||||||||||||
| Molar Mass | 279.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Kwon G, et al. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis. Oncotarget. 2017 Jun 16;8(43):74217-74232. [2]. Cha JJ, et al. APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 2017 Apr;97(4):419-431. |
APX-115 free base
CAS: 1270084-92-8 F: C17H17N3O W: 279.34
APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of
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