ML171 is a potent and selective inhibitor of NOX1, with an IC50 of 129–156 nM in cell-based assays. ML171 is not cytotoxic, and is selective among NOX family members NOX2, NOX3, and NOX4, as well as against xanthine oxidase, another cellular source of ROS. ML171 strongly blocks ROS generation in HT29 cells (IC50=0.129 μM) and only increasing over-expression of Nox1 can overcome the blockage of ROS generation caused by ML171 treatment in HEK293 cell system reconstituted with all the components required Nox1-dependent ROS generation. ML171 efficiently blocks ROS production measured by carboxy-H2-DCFDA staining as well as DPI used as a positive control.
| Cell Experiment | |
|---|---|
| Cell lines | DLD1 cells |
| Preparation method | DLD1 cells were plated on glass coverslips and after 24hrs cells were transfected with active SrcYF or empty vector (mock). 48hrs after transfection, cells were treated as indicated for 1hr with 10 μM of ML171, or with DMSO or 10 μM DPI. Afterwards, cells were fixed and stained and visualized by confocal miscroscopy. |
| Concentrations | 10 μM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 241.31 |
| Formula | C14H11NOS |
| CAS Number | 6631-94-3 |
| Solubility (25°C) | DMSO 30 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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