FCPR03
Based on 1 Customer Validation
FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.82%
- CAS 番号: 1917347-65-9
- 分子式: C15H19F2NO3
- 分子量:299.31
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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PDE4 catalytic domain 60 nM (IC50) |
PDE4B1 31 nM (IC50) |
PDE4D7 47 nM (IC50) |
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[1].
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[1].
FCPR03 (20 μM; 30 hours; HT-22 cells) treatment increases the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-22 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:30 hours
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Result:Increased cell viability in a dose-dependent manner.
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Cell Line:HT-22 cells
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Concentration:20 μM
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Incubation Time:30 hours
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Result:Reversed the effects of OGD and decreased the ratio of apoptotic cells.
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Cell Line:HT-22 cells
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Concentration:20 μM
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Incubation Time:30 hours
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Result:Increased the levels of phosphorylated AKT, glycogen synthase kinase-3β (GSK3β), and β-catenin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (250-280 g) induced middle cerebral artery occlusion (MCAO)[1]
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Dosage:1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Reduced the infarct volume and improved neurobehavioral outcomes in rats following MCAO.
化学情報
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CAS 番号 1917347-65-9
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性状 Solid
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分子量 299.31
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分子式 C15H19F2NO3
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Color White to off-white
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SMILES
O=C(NC(C)C)C1=CC=C(OC(F)F)C(OCC2CC2)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (334.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bingtian Xu, et al. FCPR03, a Novel Phosphodiesterase 4 Inhibitor, Alleviates Cerebral ischemia/reperfusion Injury Through Activation of the AKT/GSK3β/ β-catenin Signaling Pathway. Biochem Pharmacol. 2019 May;163:234-249. [Content Brief]
[2]. Zheng-Qiang Zou, et al. Novel Phosphodiesterase 4 Inhibitor FCPR03 Alleviates Lipopolysaccharide-Induced Neuroinflammation by Regulation of the cAMP/PKA/CREB Signaling Pathway and NF- κ B Inhibition. J Pharmacol Exp Ther. 2017 Jul;362(1):67-77. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3410 mL | 16.7051 mL | 33.4102 mL | 83.5254 mL |
| 5 mM | 0.6682 mL | 3.3410 mL | 6.6820 mL | 16.7051 mL | |
| 10 mM | 0.3341 mL | 1.6705 mL | 3.3410 mL | 8.3525 mL | |
| 15 mM | 0.2227 mL | 1.1137 mL | 2.2273 mL | 5.5684 mL | |
| 20 mM | 0.1671 mL | 0.8353 mL | 1.6705 mL | 4.1763 mL | |
| 25 mM | 0.1336 mL | 0.6682 mL | 1.3364 mL | 3.3410 mL | |
| 30 mM | 0.1114 mL | 0.5568 mL | 1.1137 mL | 2.7842 mL | |
| 40 mM | 0.0835 mL | 0.4176 mL | 0.8353 mL | 2.0881 mL | |
| 50 mM | 0.0668 mL | 0.3341 mL | 0.6682 mL | 1.6705 mL | |
| 60 mM | 0.0557 mL | 0.2784 mL | 0.5568 mL | 1.3921 mL | |
| 80 mM | 0.0418 mL | 0.2088 mL | 0.4176 mL | 1.0441 mL | |
| 100 mM | 0.0334 mL | 0.1671 mL | 0.3341 mL | 0.8353 mL |