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PDE4/5-IN-1

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Catalog No. T218889 Copy Product Info
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PDE4/5-IN-1 is a selective dual inhibitor of phosphodiesterase 4/5 (PDE4/5). It functionally inhibits the activities of PDE5, PDE4B2, and PDE4D2. Additionally, PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation of isolated rat prostate tissue, and reduces α-1 adrenergic receptor-mediated contraction responses in isolated rat prostate tissue. This compound also inhibits the proliferation of human hyperplastic prostate cells and can be used in research related to benign prostatic hyperplasia.

PDE4/5-IN-1

Cas No. 1807631-43-1
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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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Product Introduction

Bioactivity
Description
PDE4/5-IN-1 is a selective dual inhibitor of phosphodiesterase 4/5 (PDE4/5). It functionally inhibits the activities of PDE5, PDE4B2, and PDE4D2. Additionally, PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation of isolated rat prostate tissue, and reduces α-1 adrenergic receptor-mediated contraction responses in isolated rat prostate tissue. This compound also inhibits the proliferation of human hyperplastic prostate cells and can be used in research related to benign prostatic hyperplasia.
In vitro
PDE4/5-IN-1 (Compound VIII) (1-10 μM) exhibits dual inhibitory activity against PDE4 enzymes (specifically PDE4B2 and PDE4D2) and the PDE5 enzyme at a 1 μM concentration in a cell-free assay. At a 10 μM concentration, it also inhibits PDE6 and PDE11. At concentrations ranging from 0.003 μM to 3 μM, PDE4/5-IN-1 significantly suppresses the proliferation of human prostate cell lines RWPE-1, BPH-1, and WPMY-1, with the strongest effect on the WPMY-1 stromal cells. At 3 μM, it markedly enhances SNP-induced relaxation of rat prostate tissue and reduces contraction responses mediated by α-1 adrenergic receptors.
Chemical Properties
Molecular Weight433.41
FormulaC23H19N3O6
Cas No.1807631-43-1
SmilesO=C1C2=C(OC(C3=CC=C4OCOC4=C3)N2C(=O)CN1CCO)C5=CNC=6C=CC=CC65
Storage & Solubility Information
StoragePowder: -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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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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
Related Tags: PDE4/5-IN-1 in vitro | PDE4/5-IN-1 formula | PDE4/5-IN-1 molecular weight