Molecular Formula | C17H17N3O |
Molar Mass | 279.34 |
Density | 1.17±0.1 g/cm3(Predicted) |
Boling Point | 493.3±45.0 °C(Predicted) |
pKa | 7?+-.0.50(Predicted) |
Storage Condition | 2-8°C |
In vitro study | APX-115 free base (5 μm; 60 μm min) almost completely inhibited the expression of pro-inflammatory and fibrotic molecules in the mouse podocyte cell line induced by high glucose. In the kidney, APX-115 free base reduces Nox gene up-regulation and protein expression while improving inflammatory and fibrotic processes. |
In vivo study | APX-115 free base (oral gavage; 60 μg/kg/day; For 12 consecutive weeks) can significantly improve insulin resistance in diabetic mice. Treatment with APX-115 free base reduced urinary protein excretion and plasma creatinine levels. Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) Dosage: 60 mg/kg Administration: Oral gavage; per day; for 12 weeks Result: Significantly improved insulin resistance in diabetic mice. |
biological activity | APX-115 free base (Ewha-18278 free base) is an effective and orally active inhibitor of pan NADPH oxidase (pan-Nox). the Ki values for nox1, nox2 and nox4 are 1.08 μM, 0.57 μM and 0.63 μM respectively. APX-115 free base (Ewha-18278 free base) can significantly inhibit MCP-1/CCL2, IL-6 and TNFα in diabetic kidney. |
target | TargetValue MCP-1/CCL2 () IL-6 () TNFα () NOX2 (Cell-free say) 0.57 μM(Ki) NOX4 (Cell-free say) 0.63 μM(Ki) |
Target | Value |
MCP-1/CCL2 () | |
IL-6 () | |
TNFα () | |
NOX2 (Cell-free assay) | 0.57 μM(Ki) |
NOX4 (Cell-free assay) | 0.63 μM(Ki) |
in vitro study | APX-115 free base (5 μM; 60 min) almost completely inhibited the expression of pro-inflammatory and fibrotic molecules in mouse podocyte cell lines induced by high glucose. In the kidney, APX-115 free base attenuates Nox gene up-regulation and protein expression while improving inflammatory and fibrotic processes. |
in vivo studies | APX-115 free base (oral gavage; 60 mg/kg/day; 12 weeks) significantly improved insulin resistance in diabetic mice. APX-115 free base treatment decreased urinary protein excretion and plasma creatinine levels. Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) Dosage: 60 mg/kg Administration: Oral gavage; per day; for 12 weeks Result: Significantly improved insulin resistance in diabetic mice. |
Animal Model: | Six-week-old male diabetic db/db mice (C57BLKS/J- lepr db /lepr db ) |
Dosage: | 60 mg/kg |
Administration: | Oral gavage; per day; for 12 weeks |
Result: | Significantly improved insulin resistance in diabetic mice. |