PDE2A-IN-3
Based on 1 Customer Validation
PDE2A-IN-3 (Example Ic1) is a selective phosphodiesterase 2A (PDE2A) inhibitor with IC50s of 69 nM and 1762 nM for PDE2A and PDE10, respectively. PDE2A-IN-3 can be used for the study of neurological and psychiatric disorders.
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- Pureté : 99.88%
- CAS No.: 1426833-08-0
- Formule: C15H10ClN5
- Masse moléculaire:295.73
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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
Activité biologique
Description
IC50 & Target
[1]|
PDE2A 69 nM (IC50) |
PDE10 1762 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
6920 nM
Compound: 6
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Inhibition of full length human PDE11A4 expressed in HEK cells by scintillation proximity assay
Inhibition of full length human PDE11A4 expressed in HEK cells by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
>10000 nM
Compound: 6
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Inhibition of 6-His-tagged human recombinant PDE7A1 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE7A1 expressed in Sf9 cells by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
>10000 nM
Compound: 6
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Inhibition of 6-His-tagged human recombinant PDE9A1 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE9A1 expressed in Sf9 cells by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
29 nM
Compound: 6
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Inhibition of 6-His-tagged human recombinant PDE2A expressed in Sf9 cells using [3H]cGMP incubated for 40 mins by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE2A expressed in Sf9 cells using [3H]cGMP incubated for 40 mins by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
480 nM
Compound: 6
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Inhibition of 6-His-tagged rat recombinant PDE10A expressed in Sf9 cells using [3H]cAMP incubated for 60 mins by scintillation proximity assay
Inhibition of 6-His-tagged rat recombinant PDE10A expressed in Sf9 cells using [3H]cAMP incubated for 60 mins by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
5890 nM
Compound: 6
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Inhibition of 6-His-tagged human recombinant PDE4D3 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE4D3 expressed in Sf9 cells by scintillation proximity assay
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[PMID: 25815146] |
| Sf9 | IC50 |
>10000 nM
Compound: 6
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Inhibition of 6-His-tagged human recombinant PDE5A3 expressed in Sf9 cells by scintillation proximity assay
Inhibition of 6-His-tagged human recombinant PDE5A3 expressed in Sf9 cells by scintillation proximity assay
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[PMID: 25815146] |
In Vitro
Phosphodiesterase 2A (PDE2A) is a dual substrate enzyme with higher affinity for cGMP although it may metabolize either cAMP or cGMP depending on the tissue. cAMP is derived from adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway. Although expressed in the periphery, the highest expression levels of PDE2A are in the brain.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1426833-08-0
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Appearance Solid
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Masse moléculaire 295.73
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Formule C15H10ClN5
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Color Off-white to brown
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SMILES
CC1=NC2=C(C=NC=C2)N3C1=NN=C3C4=CC=CC=C4Cl
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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
In Vitro:
DMSO : 12.5 mg/mL (42.27 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (4.23 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (4.23 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (282 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
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 | 3.3815 mL | 16.9073 mL | 33.8146 mL | 84.5366 mL |
| 5 mM | 0.6763 mL | 3.3815 mL | 6.7629 mL | 16.9073 mL | |
| 10 mM | 0.3381 mL | 1.6907 mL | 3.3815 mL | 8.4537 mL | |
| 15 mM | 0.2254 mL | 1.1272 mL | 2.2543 mL | 5.6358 mL | |
| 20 mM | 0.1691 mL | 0.8454 mL | 1.6907 mL | 4.2268 mL | |
| 25 mM | 0.1353 mL | 0.6763 mL | 1.3526 mL | 3.3815 mL | |
| 30 mM | 0.1127 mL | 0.5636 mL | 1.1272 mL | 2.8179 mL | |
| 40 mM | 0.0845 mL | 0.4227 mL | 0.8454 mL | 2.1134 mL |
PDE2A-IN-3 Related Classifications
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