1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. FCPR03

FCPR03 

Cat. No.: HY-117977
Handling Instructions

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.

For research use only. We do not sell to patients.

FCPR03 Chemical Structure

FCPR03 Chemical Structure

CAS No. : 1917347-65-9

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Description

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[1][2].

IC50 & Target[1]

PDE4 catalytic domain

60 nM (IC50)

PDE4B1

31 nM (IC50)

PDE4D7

47 nM (IC50)

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[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].

Cell Viability Assay[1]

Cell 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 Analysis[1]

Cell 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 Analysis[1]

Cell 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[1].

Animal Model: Adult male Sprague-Dawley rats (250-280 g) induced middle cerebral artery occlusion (MCAO)[1]
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.
Molecular Weight

299.31

Formula

C₁₅H₁₉F₂NO₃

CAS No.

1917347-65-9

SMILES

O=C(NC(C)C)C1=CC=C(OC(F)F)C(OCC2CC2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

FCPR03FCPR 03FCPR-03Phosphodiesterase (PDE)PDE4ischemicstrokeantidepressant-likeneuroprotectiveAKTGSK3ββ-cateninanti-inflammatoryPDE4B1PDE4D7Inhibitorinhibitorinhibit

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