PDE9-IN-1
Based on 1 Customer Validation
PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.70%
- CAS No.: 2305087-92-5
- Formule: C17H23FN6O2
- Masse moléculaire:362.40
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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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PDE9A 8.7 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>30 μM
Compound: 2
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Inhibition of human ERG expressed in CHO cells by patch clamp assay
Inhibition of human ERG expressed in CHO cells by patch clamp assay
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[PMID: 30916555] |
| Sf9 | IC50 |
>10000 nM
Compound: 2
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Inhibition of recombinant human N-terminal GST-tagged PDE1C (2 to 634 residues) expressed in baculovirus infected Sf9 cells using 3H-cGMP as substrate after 15 mins by liquid scintillation counting method
Inhibition of recombinant human N-terminal GST-tagged PDE1C (2 to 634 residues) expressed in baculovirus infected Sf9 cells using 3H-cGMP as substrate after 15 mins by liquid scintillation counting method
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[PMID: 30916555] |
PDE9-IN-1 is excellent selectivity across PDE families[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Unilateral common carotid artery occlusion (UCCAO) mouse model[1]
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Dosage:2.5 and 5.0 mg/kg
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Administration:Oral administration; daily for 21 days
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Result:Significantly reduced the day 6 escape latency time and increased the frequency of platform area crossings, and recovered learning and memory function. High dose group possibly improved the escape latency time of mice.
Chemical Information
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CAS No. 2305087-92-5
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Appearance Solid
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Masse moléculaire 362.40
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Formule C17H23FN6O2
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Color White to off-white
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SMILES
O=C1C2=C(N(C3CCCC3)N=C2)N=C(N[C@H](C)C(N4CC[C@H](F)C4)=O)N1
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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 : 100 mg/mL (275.94 mM; Need ultrasonic; 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)
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: ≥ 2.5 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (273 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 |
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| DMSO | 1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL | 68.9845 mL |
| 5 mM | 0.5519 mL | 2.7594 mL | 5.5188 mL | 13.7969 mL | |
| 10 mM | 0.2759 mL | 1.3797 mL | 2.7594 mL | 6.8985 mL | |
| 15 mM | 0.1840 mL | 0.9198 mL | 1.8396 mL | 4.5990 mL | |
| 20 mM | 0.1380 mL | 0.6898 mL | 1.3797 mL | 3.4492 mL | |
| 25 mM | 0.1104 mL | 0.5519 mL | 1.1038 mL | 2.7594 mL | |
| 30 mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 2.2995 mL | |
| 40 mM | 0.0690 mL | 0.3449 mL | 0.6898 mL | 1.7246 mL | |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5519 mL | 1.3797 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3449 mL | 0.8623 mL | |
| 100 mM | 0.0276 mL | 0.1380 mL | 0.2759 mL | 0.6898 mL |
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