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Phosphodiesterase-IN-5
Catalog No. T213833 Copy Product Info
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Phosphodiesterase-IN-5 is a potent and orally bioavailable selective phosphodiesterase 10A (PDE10A) inhibitor, with an IC50 value of 6.2 nM. It demonstrates over 1612-fold selectivity for other PDE subtypes. By blocking the cAMP/PKA/CREB signaling pathway, it inhibits myofibroblast differentiation and shows significant antifibrotic effects in a Bleomycin (BLM)-induced mouse model of pulmonary fibrosis (PF). Phosphodiesterase-IN-5 is applicable for pulmonary fibrosis research.
Phosphodiesterase-IN-5
Copy Product Info🥰Excellent
Catalog No. T213833
Phosphodiesterase-IN-5 is a potent and orally bioavailable selective phosphodiesterase 10A (PDE10A) inhibitor, with an IC50 value of 6.2 nM. It demonstrates over 1612-fold selectivity for other PDE subtypes. By blocking the cAMP/PKA/CREB signaling pathway, it inhibits myofibroblast differentiation and shows significant antifibrotic effects in a Bleomycin (BLM)-induced mouse model of pulmonary fibrosis (PF). Phosphodiesterase-IN-5 is applicable for pulmonary fibrosis research.
Phosphodiesterase-IN-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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| Description | Phosphodiesterase-IN-5 is a potent and orally bioavailable selective phosphodiesterase 10A (PDE10A) inhibitor, with an IC50 value of 6.2 nM. It demonstrates over 1612-fold selectivity for other PDE subtypes. By blocking the cAMP/PKA/CREB signaling pathway, it inhibits myofibroblast differentiation and shows significant antifibrotic effects in a Bleomycin (BLM)-induced mouse model of pulmonary fibrosis (PF). Phosphodiesterase-IN-5 is applicable for pulmonary fibrosis research. |
| Targets&IC50 | PDE10A:6.2 nM |
| In vitro | Phosphodiesterase-IN-5 (compound QC-3) (5-20 μM; 48 hours) exhibits antifibrotic activity in TGF-β1-stimulated MRC-5 cells by activating the cAMP/PKA/CREB pathway, which inhibits myofibroblast differentiation and ECM deposition. Phosphodiesterase-IN-5 binds to the PDE10A catalytic domain, forming a hydrogen bond with Gln726 and a hydrophobic interaction with Ile692, while the 6-F substituent forms a halogen bond with Asp674 via a water molecule. |
| In vivo | Phosphodiesterase-IN-5 (10 mg/kg, oral gavage, once daily for 21 days) demonstrates significant antifibrotic activity by inhibiting myofibroblast differentiation through the cAMP/PKA/CREB signaling pathway in a BLM-induced mouse model of pulmonary fibrosis. |
| 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.
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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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