2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. P7-2104

P7-2104 is a selective CNS-penetrant PDE7A inhibitor with an IC50 of of 31 nM. P7-2104 exhibits selectivity over hERG channels and most CYP450 isoforms. P7-2104 can be used for PDE7-targeted PET neuroimaging, and for the research of neurodegenerative disorders.

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

P7-2104

P7-2104 Chemical Structure

CAS No. : 460346-02-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

P7-2104 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

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Description

P7-2104 is a selective CNS-penetrant PDE7A inhibitor with an IC50 of of 31 nM. P7-2104 exhibits selectivity over hERG channels and most CYP450 isoforms. P7-2104 can be used for PDE7-targeted PET neuroimaging, and for the research of neurodegenerative disorders[1].

IC50 & Target[1]

PDE7A

31 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.01 μM
Compound: 7
Inhibition of human PDE7A1 expressed in baculovirus infected Sf9 cells
Inhibition of human PDE7A1 expressed in baculovirus infected Sf9 cells
[PMID: 15324877]
In Vitro

P7-2104 does not inhibit the hERG channel (IC50 > 100 μM), weakly inhibits CYP1A2 (IC50 = 4.4 μM), and does not significantly interact with other CYP450 isoforms (IC50 ≥ 10 μM)[1].
P7-2104 has free plasma fractions of ~2.8% in mouse, ~2.2% in rat, and ~1.4% in human plasma[1].

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

P7-2104 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration
Rat[1] 1 mg/kg i.v. 39.39 ng/mL 131.68 ng/g
Rat[1] 1 mg/kg i.v. 229.06 ng/mL 876.42 ng/g
Rat[1] 1 mg/kg i.v. 712.49 ng/mL 3316.17 ng/g
Molecular Weight

280.75

Formula

C14H17ClN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1)NC2=C(C31CCCCC3)C(OC)=CC=C2Cl
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 : 5.83 mg/mL (20.77 mM; ultrasonic and warming and heat to 60°C; 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 3.5619 mL 17.8094 mL 35.6189 mL
5 mM 0.7124 mL 3.5619 mL 7.1238 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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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
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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 3.5619 mL 17.8094 mL 35.6189 mL 89.0472 mL
5 mM 0.7124 mL 3.5619 mL 7.1238 mL 17.8094 mL
10 mM 0.3562 mL 1.7809 mL 3.5619 mL 8.9047 mL
15 mM 0.2375 mL 1.1873 mL 2.3746 mL 5.9365 mL
20 mM 0.1781 mL 0.8905 mL 1.7809 mL 4.4524 mL
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P7-2104 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:

P7-2104460346-02-5Phosphodiesterase (PDE)PDE7blood-brain barrierCYP1A2hERG channelsPhe377Phe345PDE7ATyr172CYP450 isoformsPDE7BInhibitorinhibitorinhibit

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