1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PDE2A-IN-2

PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases .

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PDE2A-IN-2

PDE2A-IN-2 Chemical Structure

CAS No. : 2055901-03-4

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Description

PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases [1].

IC50 & Target[1]

PDE2A

5.49 nM (Ki)

In Vitro

PDE2A-IN-2 (compound 1) (1 μM, 30 min) reduces the radiotracer signal in PDE2A-rich regions, leading to a more homogeneous distribution in SD rat brain sections when co-treated with its unlabeled form (1 μM) [1].

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

In Vivo

PDE2A-IN-2 (compound 1) (1 mg/kg, i.v., once) exhibits low binding affinity in SD rat[1].

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

Animal Model: SD rat[1]
Dosage: 1 mg/kg
Administration: i.v., once
Result: Led to similar TAC patterns and regional brain distributions to baseline.
Molecular Weight

347.34

Formula

C17H16F3N5

CAS No.
SMILES

CC1=NC2=C(C(NC3(C4=CC=C(C=C4)C(F)(F)F)CC3)=N1)C=NN2C

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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PDE2A-IN-2
Cat. No.:
HY-180526
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