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APX-115 (Ewha-18278) 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 effectively prevents kidney injury[1]. | [in vivo]
APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice[2].
APX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels[2].
| Animal Model: | Six-week-old male diabetic db/db mice (C57BLKS/J-leprdb/leprdb)[2] | | Dosage: | 60?mg/kg | | Administration: | Oral gavage; per day; for 12 weeks | | Result: | Significantly improved insulin resistance in diabetic mice.
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| [IC 50]
NOX1; NOX2; NOX4 | [References]
[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. DOI:10.18632/oncotarget.18540
[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. DOI:10.1038/labinvest.2017.2 |
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