PDE3/4-IN-2
Based on 1 Customer Validation
PDE3/4-IN-2 is a dual PDE3A and PDE4B1 inhibitor, with an IC50 of 0.13 nM against PDE3A and 50 nM against PDE4B1. PDE3/4-IN-2 exhibits higher systemic exposure and longer retention time in lung tissues in ICR mice. PDE3/4-IN-2 can be used in research on respiratory diseases such as asthma and chronic obstructive pulmonary disease, as well as autoimmune inflammation-related studies.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 2857007-03-3
- Formula: C28H33N5O4
- Molecular Weight:503.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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PDE3A 0.13 nM (IC50) |
PDE4B1 50 nM (IC50) |
PDE3/4-IN-2 (Compound 1) (at 500 nM for PDE3A and 2000 nM for PDE4B1) exhibits an inhibition rate of 100.3% against PDE3A and 82.8% against PDE4B1[1].
PDE3/4-IN-2 (0.005-10000 nM; 15 min (with enzyme); 30 min (with FAM-cAMP); 60 min (with detection solution)) potently inhibits the activity of purified PDE4B1 enzyme, with an IC50 of 50 nM[1].
PDE3/4-IN-2 (0.005-10000 nM; 15 min (with enzyme); 30 min (with FAM-cAMP); 60 min (with detection solution)) potently inhibits the activity of purified PDE3A enzyme, with an IC50 of 0.13 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2857007-03-3
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Appearance Solid
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Molecular Weight 503.59
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Formula C28H33N5O4
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Color White to off-white
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SMILES
O=C1N=C(N(CCN2C(NCC2)=O)C3=C(C)C=C(C)C=C3C)C=C4C5=C(CCN14)C=C(OC)C(OC)=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 12.5 mg/mL (24.82 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)
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 (2.48 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 1.9857 mL | 9.9287 mL | 19.8574 mL | 49.6436 mL |
| 5 mM | 0.3971 mL | 1.9857 mL | 3.9715 mL | 9.9287 mL | |
| 10 mM | 0.1986 mL | 0.9929 mL | 1.9857 mL | 4.9644 mL | |
| 15 mM | 0.1324 mL | 0.6619 mL | 1.3238 mL | 3.3096 mL | |
| 20 mM | 0.0993 mL | 0.4964 mL | 0.9929 mL | 2.4822 mL |