TAK-915
Based on 1 Customer Validation
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
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- Pureté: 99.57%
- CAS No.: 1476727-50-0
- Formule: C19H18F4N4O5
- Masse moléculaire:458.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PDE2A 0.61 nM (IC50) |
PDE1A 2497 nM (IC50) |
TAK-915 (1, 3, and 10 mg/kg, p.o.) dose-dependently attenuates the non-selective muscarinic antagonist scopolamine-induced memory deficits in rats[2].
Oral dosing of TAK-915 (compound 36) (3 or 10 mg/kg) in mice produces a dose-dependent increase in 3',5'-cyclic guanosine monophosphate (cGMP) levels, with significant cGMP increases observed at a dose of 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male F344 rats (10-week-old and 26-month-old) bearing morris water maze task[2]
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Dosage:3 mg/kg
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Administration:Oral administration; daily; for 4 days
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Result:Significantly reduced escape latency in aged rats in the Morris water maze task.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1476727-50-0
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Appearance Solid
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Masse moléculaire 458.36
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Formule C19H18F4N4O5
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Color Light yellow to yellow
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SMILES
O=C(N1)CN(C(N[C@@H](C2=CC(F)=C(OC(F)(F)F)C=C2)COC)=O)C3=C1C=C(OC)C=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 7.5 mg/mL (16.36 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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Mikami S, et al. Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem. 2017 Sep 28;60(18):7677-7702. [Content Brief]
[2]. Nakashima M, et al. TAK-915, a phosphodiesterase 2A inhibitor, ameliorates the cognitive impairment associated with aging in rodent models. Behav Brain Res. 2019 Dec 30;376:112192. [Content Brief]
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 | 2.1817 mL | 10.9085 mL | 21.8169 mL | 54.5423 mL |
| 5 mM | 0.4363 mL | 2.1817 mL | 4.3634 mL | 10.9085 mL | |
| 10 mM | 0.2182 mL | 1.0908 mL | 2.1817 mL | 5.4542 mL | |
| 15 mM | 0.1454 mL | 0.7272 mL | 1.4545 mL | 3.6362 mL |
TAK-915 Related Classifications
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