1. Metabolic Enzyme/Protease TGF-beta/Smad Stem Cell/Wnt
  2. Phosphodiesterase (PDE) PKA
  3. PDE2-IN-1

PDE2-IN-1 is a potent and orally active PDE2 inhibitor with an IC50 of 0.6 μM, demonstrating neuroprotective effects. PDE2-IN-1 modulates the PKA/CREB/BDNF signaling pathway by inhibiting PDE2. PDE2-IN-1 improves memory deficits and cognitive impairment in an okadai acid (OKA)-induced Alzheimer’s disease (AD) mouse model. PDE2-IN-1 can be used for the research of AD.

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

PDE2-IN-1

PDE2-IN-1 Chemical Structure

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Description

PDE2-IN-1 is a potent and orally active PDE2 inhibitor with an IC50 of 0.6 μM, demonstrating neuroprotective effects. PDE2-IN-1 modulates the PKA/CREB/BDNF signaling pathway by inhibiting PDE2. PDE2-IN-1 improves memory deficits and cognitive impairment in an okadai acid (OKA)-induced Alzheimer’s disease (AD) mouse model. PDE2-IN-1 can be used for the research of AD[1].

IC50 & Target[1]

PDE2

0.6 μM (IC50)

In Vitro

PDE2-IN-1 (compound 14c) (0-50 μM; 24 h) shows no cytotoxicity in neuronal cells (U251, SY5Y, and HMC3 cells)[1].

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

Cell Viability Assay[1]

Cell Line: U251, SY5Y, and HMC3 cell lines
Concentration: 0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM
Incubation Time: 24 h
Result: Showed no effects on U251, SY5Y, and HMC3 cell survival rates.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Vz-F_obs CL/F Cmax F
Rat[1] 2 mg/kg i.v. 3540.2 μg/L·h 3560.228 μg/L·h 4.292 h 4.481 h 4.437 h 0.083 h 3.493 L/kg 0.584 L/h/kg 1519.1 μg/L /
Rat[1] 20 mg/kg p.o. 34006.498 μg/L·h 34057.752 μg/L·h 7.856 h 7.916 h 4.418 h 2.167 h 3.748 L/kg 0.598 L/h/kg 3547.8 μg/L 95.66 %
In Vivo

PDE2-IN-1 (10 and 30 mg/kg, i.p., daily for 14 dyas) improves memory deficits and cognitive impairment in an OKA-induced AD mouse model[1].

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

Animal Model: C57BL/6 mice (20-30 g) bilateral intracerebroventricularly injected with OKA[1]
Dosage: 10 and 30 mg/kg
Administration: i.p., daily for 14 days
Result: Had a negligible effect on the mean daily bodyweight profile in OKA-induced AD mice.
Showed no obvious changes of the levels of serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), carbamide (UREA), creatinine (CREA) and AST/ALT ratio in OKA-induced AD group and different doses group.
Led to minimal injury to hippocampal neurons.
Showed beneficial effects to ameliorate the memory and cognitive impairment in OKA-induced AD mice.
Ameliorated OKA-induced memory and cognitive impairment via PKA/CREB/BDNF pathway.
Alleviated synaptic impairments in OKA-induced AD mice.
Molecular Weight

396.36

Formula

C18H19F3N4O3

SMILES

O=C1C2=NN(CCO)C(C(NC(C3=CC=C(C(F)(F)F)C=C3)C)=O)=C2CCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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.

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Product Name:
PDE2-IN-1
Cat. No.:
HY-179337
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