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PDE3/4-IN-4
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Catalog No. T218257 Copy Product Info
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PDE3/4-IN-4 is an orally active inhibitor targeting both PDE3A and PDE4B with an IC₅₀ of 10 nM for PDE3A and 9.4 nM for PDE4B, demonstrating selective activity compared to most other PDE family members. It modulates the cAMP/PKA/CREB signaling pathway, inhibits the pro-inflammatory factor IL-6, and reduces the expression of inflammatory markers in liver tissue. PDE3/4-IN-4 alleviates liver fibrosis and limits liver injury in mouse models of cholestasis and sepsis-induced liver damage. This compound is applicable in studies related to liver injury, cholestatic liver disease, and sepsis-induced liver damage.
PDE3/4-IN-4
Cas No. 3088024-27-2
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PDE3/4-IN-4 is an orally active inhibitor targeting both PDE3A and PDE4B with an IC₅₀ of 10 nM for PDE3A and 9.4 nM for PDE4B, demonstrating selective activity compared to most other PDE family members. It modulates the cAMP/PKA/CREB signaling pathway, inhibits the pro-inflammatory factor IL-6, and reduces the expression of inflammatory markers in liver tissue. PDE3/4-IN-4 alleviates liver fibrosis and limits liver injury in mouse models of cholestasis and sepsis-induced liver damage. This compound is applicable in studies related to liver injury, cholestatic liver disease, and sepsis-induced liver damage. |
| Targets & IC50 | PDE3A:10 nM |
| In vitro | PDE3/4-IN-4 (compound D5), at concentrations up to 60 μM with a 24-hour exposure, shows no significant toxicity to normal human liver cells (LO2). It inhibits IL-6 secretion in LO2 cells stimulated by Lipopolysaccharides (LPS) with an IC₅₀ of 14.89 μM. Pre-treatment with PDE3/4-IN-4 (compound D5) at 15 μM for 12 hours before LPS stimulation increases the expression of p-CREB and p-PKA in LO2 cells. This compound also demonstrates substantial metabolic stability in liver microsomes from mice, rats, dogs, monkeys, and humans. |
| In vivo | PDE3/4-IN-4 (compound D5), administered at 10-40 mg/kg via gavage once daily for 7 consecutive days, can alleviate liver inflammation and fibrosis in mice subjected to bile duct ligation (BDL), with the 40 mg/kg dose showing superior efficacy. Similarly, PDE3/4-IN-4 at the same dosage and regimen reduces liver inflammation and injury in mice undergoing cecal ligation and puncture (CLP), with the greatest effectiveness observed at the 40 mg/kg dosage. |
| Molecular Weight | 559.56 |
| Formula | C30H27F2N5O4 |
| Cas No. | 3088024-27-2 |
| Smiles | O=C(NC=1C=CC(=CC1)C2=NNC(=O)CC2C)C=3C=CC=C4N=C(NC43)C=5C=CC(OC(F)F)=C(OCC6CC6)C5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: PDE3/4-IN-4 in vivo | PDE3/4-IN-4 in vitro | PDE3/4-IN-4 formula | PDE3/4-IN-4 molecular weight
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