GKT137831 (Setanaxib) attenuated hypoxia-induced H(2)O(2) release, proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs in vitro.
In vivo GKT137831 inhibited hypoxia-induced increases in TGF-β1 and reductions in PPARγ expression and attenuated RVH and pulmonary artery wall thickness but not increases in RVSP or muscularization of small arterioles.Targeting Nox4 with GKT137831 provides a novel strategy to attenuate hypoxia-induced alterations in pulmonary vascular wall cells that contribute to vascular remodeling and RVH, key features involved in PH pathogenesis. GKT137831, attenuated liver fibrosis and ROS production in both SOD1mu and WT mice as well as messenger RNA expression of fibrotic and NOX genes. Treatment with GKT137831 suppressed ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT HSCs.
FASEB J. 2021 Apr;35(4):e21531.
Inhibition of NADPH oxidase 4 attenuates lymphangiogenesis and tumor metastasis in breast cancer
GKT137831 (Setanaxib) purchased from AbMole
J Sex Med. 2021 Dec;18(12):1970-1983.
NOX1/4 Inhibitor GKT-137831 Improves Erectile Function in Diabetic Rats by ROS Reduction and Endothelial Nitric Oxide Synthase Reconstitution
GKT137831 (Setanaxib) purchased from AbMole
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Source | Cell Physiol Biochem (2018). Figure 5. GKT137831 |
| Method | DCF assays | |
| Cell Lines | AML12 cells | |
| Concentrations | 0.2, 1 and 5 μM | |
| Incubation Time | 1 h | |
| Results | Importantly, the application of GKT137381 dose-dependently decreased the percentage of PA-induced apoptosis in cultured AML12 cells |
| Molecular Weight | 394.85 |
| Formula | C21H19ClN4O2 |
| CAS Number | 1218942-37-0 |
| Solubility (25°C) | DMSO 10 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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