GSK2795039 is the first small molecule NADPH oxidase 2 (NOX2) inhibitor, with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 shows activity in a murine model of acute pancreatitis, GSK2795039 (100 mg/kg; i.p.) decreases activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.
| Cell Experiment | |
|---|---|
| Cell lines | BV2 microglia cell |
| Preparation method | Experimental groups were treated with FeSO4 tetrahydrate (100 μM), LPS serotype 026:B6 (100 ng/ml), ferrous ammonium sulfate (Fe(NH4)2(SO4)2) (100 μM), (sodium sulfate) Na2SO4 (100 μM), or DFO (250 μM). All treatments were added simultaneously and all tests were performed 24 h after treatment. In subsequent experiments, microglia were treated with GKT137831 (50 μM), GSK2795039 (25 μM), or vehicle dimethyl sulfoxide (DMSO) (≤ 1%). These treatments were given simultaneously to the cultures and all assays were conducted 24 h afterwards. |
| Concentrations | 25 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley (SD) rats, C57BL6/J mice, gp91phox knockout mice |
| Formulation | dissolved in 20% DMSO, 20% Tween 80, 60% polyethylene glycol 200, dose volume of 2 ml/kg |
| Dosages | 2-100 mg/kg |
| Administration | i.p. injection |
| Molecular Weight | 450.56 |
| Formula | C23H26N6O2S |
| CAS Number | 1415925-18-6 |
| 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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