Description
FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC 50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effectsIn VitroFCPR03 (5-20 µM; 30 hours; HT-22 cells) treatment increases cell viability (oxygen-glucose deprivation (OGD)-induced) in a dose-dependent manner, and 10 µM FCPR03 shows significant protective effects. FCPR03 (20 µM; 30 hours; HT-22 cells) treatment protects against OGD-induced cellular apoptosis in both HT-22 cells and cortical neurons. The levels of mitochondrial membrane potential (MMP) and ROS are also restored by FCPR03. FCPR03 (20 µM; 30 hours; HT-22 cells) treatment increases the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HT-22 cells Concentration: 5 µM, 10 µM, 20 µM Incubation Time: 30 hours Result: Increased cell viability in a dose-dependent manner. Apoptosis AnalysisCell Line: HT-22 cells Concentration: 20 µM Incubation Time: 30 hours Result: Reversed the effects of OGD and decreased the ratio of apoptotic cells. Western Blot AnalysisCell Line: HT-22 cells Concentration: 20 µM Incubation Time: 30 hours Result: Increased the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin.In VivoFCPR03 (1.25-5 mg/kg; intraperitoneal injection; once; adult male Sprague-Dawley rats) treatment reduces the infarct volume and improves neurobehavioral outcomes in rats following MCAO. FCPR03 increases the levels of phosphorylated AKT, GSK3β and β-catenin within the ischemic penumbra of rats following cerebral ischemia-reperfusion. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult male Sprague-Dawley rats (250-280 g) induced middle cerebral artery occlusion (MCAO) Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg Administration: Intraperitoneal injection; once Result: Reduced the infarct volume and improved neurobehavioral outcomes in rats following MCAO.Form:SolidIC50& Target:PDE4 catalytic domain 60 nM (IC 50 ) PDE4B1 31 nM (IC 50 ) PDE4D7 47 nM (IC 50 )