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

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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FCPR03 Chemical Structure

FCPR03 Chemical Structure

CAS No. : 1917347-65-9

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Based on 1 publication(s) in Google Scholar

FCPR03 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FCPR03 Related Antibodies

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].

MedChemExpress (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)[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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3410 mL 16.7051 mL 33.4102 mL
5 mM 0.6682 mL 3.3410 mL 6.6820 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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FCPR03 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FCPR031917347-65-9FCPR 03FCPR-03Phosphodiesterase (PDE)PDE4ischemicstrokeantidepressant-likeneuroprotectiveAKTGSK3ββ-cateninanti-inflammatoryPDE4B1PDE4D7Inhibitorinhibitorinhibit

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