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.
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- 화학식: C18H19F3N4O3
- 분자량:396.36
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PDE2 0.6 μM (IC50) |
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.
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Cell Line:U251, SY5Y, and HMC3 cell lines
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Concentration:0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM
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Incubation Time:24 h
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Result:Showed no effects on U251, SY5Y, and HMC3 cell survival rates.
| 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 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (20-30 g) bilateral intracerebroventricularly injected with OKA[1]
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Dosage:10 and 30 mg/kg
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Administration:i.p., daily for 14 days
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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.
Chemical Information
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분자량 396.36
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화학식 C18H19F3N4O3
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SMILES
O=C1C2=NN(CCO)C(C(NC(C3=CC=C(C(F)(F)F)C=C3)C)=O)=C2CCN1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE2-IN-1 Related Classifications
HY-179337 Related Classifications
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