APX-115 is a potent, orally active inhibitor of pan NADPH oxidase (Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line.
APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice.
| Molecular Weight | 279.34 |
| Formula | C17H17N3O |
| CAS Number | 1270084-92-8 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related NADPH Oxidase Products |
|---|
| Fluoflavine
Fluoflavine is a selective NOX1 inhibitor with an IC50 value of 90 nM.Fluoflavine is >100 times more selective for NOX1 than NOX2, NOX3, NOX4, and has an IC50 >10 μM for all of them.Fluoflavine was shown to be a selective inhibitor of NOX1 with an IC50 of 360 nM in HEK293 cells. |
| NoxA1ds
NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. |
| GLX481369
GLX481369 is a redox active substance. |
| Noxa B BH3
Noxa B BH3 is a biological active peptide. |
| Noxa A BH3
Noxa A BH3 is a biological active peptide. |
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