名称 | FCPR03 |
描述 | FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects. |
体外活性 | FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). In HT-22 cells, FCPR03 (5, 10, and 20 μM) increases cell viability under the oxygen-glucose deprivation (OGD) induced condition in a dose-dependent manner. FCPR03 (20 μM) increases the levels of phosphorylated AKT, GSK-3β, and β-catenin. FCPR03 (20 μM) protects against OGD-induced cellular apoptosis in both HT-22 cells and cortical neurons. The levels of mitochondrial membrane potential (MMP) and ROS are restored by FCPR03. FCPR03 (10 μM) shows significant protective effects[2]. |
体内活性 | In adult male Sprague-Dawley rats following cerebral ischemia-reperfusion, FCPR03 increases the levels of phosphorylated AKT, GSK3β and β-catenin within the ischemic penumbra. In rats following MCAO, FCPR03 (1.25, 2.5, 5 mg/kg; i.p.) reduces the infarct volume and improves neurobehavioral outcomes[2]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 95 mg/mL (317.40 mM), Sonication is recommended.
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关键字 | antidepressant-like | PDE4B1 | PDE4D7 | FCPR-03 | PDE4 | neuroprotective | ischemic | AKT | GSK3β | FCPR 03 | FCPR03 | inhibit | anti-inflammatory | Phosphodiesterase (PDE) | β-catenin | Inhibitor | stroke |
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