FCPR03
规格
| Cas Number | 1917347-65-9(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | Phosphodiesterase (PDE),Metabolic Enzyme/Protease,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | FCPR03 是一种强效的选择性磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4 催化域、PDE4B1 和 PDE4D7 的 IC 50 值分别为 60 nM、31 nM 和 47 nM。与其他 PDE（PDE1-3 和 PDE5）相比，FCPR03 显示出至少 2100 倍的选择性。 |
| 英文描述 |
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 effects In Vitro FCPR03 (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 Vivo FCPR03 (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. IC50& Target:PDE4 catalytic domain 60 nM (IC 50 ) PDE4B1 31 nM (IC 50 ) PDE4D7 47 nM (IC 50 ) |