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GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $29 | - | In Stock |
| Description | GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production. |
| Targets&IC50 | NOX1:160 nM (Ki), NOX4:165 nM (Ki) |
| In vitro | GKT136901 hydrochloride is a potent, selective and orally active NADPH oxidase (NOX1/4) inhibitor with Ki values of 160 nM and 165 nM, respectively. [1] GKT136901 hydrochloride significantly reduced the production of superoxide radical anion and H2O2 in MPT cells induced by high D-glucose and eliminated the effect of high D-glucose on p38MAP kinase activation in MPT cells after treatment with GKT136901 hydrochloride at a dose of 10 μM for 30 min. [3] GKT136901 hydrochloride attenuated methamphetamine (METH)-induced oxidative stress in HBMEC treated at a dose of 10 μM for 2 hours and effectively protected HBMEC from METH-induced blood-brain barrier (BBB) dysfunction. [5] |
| In vivo | GKT136901 hydrochloride exhibited nephroprotective effects in a mouse model of type 2 diabetes mellitus when administered orally at a dose of 30-90 mg/kg daily for 16 weeks. [6] |
| Synonyms | GKT-901 hydrochloride, GKT-771 hydrochloride, GKT-136901 hydrochloride, AK120765 hydrochloride, AK 120765 hydrochloride |
| Molecular Weight | 403.26 |
| Formula | C19H16Cl2N4O2 |
| Cas No. | 1254507-01-1 |
| Smiles | Cl.O=C1C=C2NN(C(=O)C2=C(N1CC3=NC=CC=C3)C)C=4C=CC=CC4Cl |
| Relative Density. | no data available |
| Color | Yellow |
| Appearance | Solid |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 2 mg/mL (4.96 mM), Sonication is recommended. DMSO: 50 mg/mL (123.99 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.96 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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