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Vesnarinone
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Catalog No. T3465Cas No. 81840-15-5
Alias Piteranometozine, OPC-8212, Arkin
Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.
Vesnarinone
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Purity: 98.13%
Catalog No. T3465Alias Piteranometozine, OPC-8212, ArkinCas No. 81840-15-5
Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $73 | In Stock | In Stock | |
| 25 mg | $119 | In Stock | In Stock | |
| 50 mg x 5 mM (in DMSO) | $221 | In Stock | In Stock | |
| 100 mg | $329 | - | In Stock | |
| 200 mg | $475 | - | In Stock | |
| 1 mL x 5 mM (in DMSO) | $42 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.13%
Color:White
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Product Introduction
Vesnarinone AI Summary
Vesnarinone exhibits diverse bioactivities, including significant inhibitory effects on various enzymes and receptors. It inhibits cyclic AMP phosphodiesterase from human platelets with an IC50 value of 6200.0 nM and shows a high IC50 ratio for inhibiting platelet aggregation (ratio of 608.0). It also competes against crude canine cardiac cAMP phosphodiesterase (IC50 = 32000.0 nM) and inhibits the cAMP Phosphodiesterase enzyme with 87.0% efficiency.
The compound inhibits the human Potassium channel HERG expressed in mammalian cells with an IC50 value of 1096.48 nM and shows similar activity against human ERG expressed in CHO cells. Vesnarinone inhibits the IKr potassium channel with an IC50 value of 18000.0 nM and exhibits inhibitory activity on human PDE3A and PDE3B with IC50 values of 10700.0 nM and 13200.0 nM, respectively.
Cardiotonic effects and increased contractile force are observed in ferret papillary muscle (C20 = 2.3 uM) and isolated reserpine-treated Wistar rat whole atrium, showing positive inotropic and chronotropic activities at concentrations ranging from 1 uM to 100 uM. Additionally, it shows moderate liver toxicity with a 0.4% incident rate of elevated serum activity levels of ALT or AST during clinical trials and has been linked to antiviral activity against SARS-CoV-2 with varying inhibition rates.
Furthermore, Vesnarinone inhibits human HDAC6 enzyme activity, implying potential HDAC6 inhibitory bioactivity. Finally, it has shown binding affinity towards multiple receptors and enzymes, but without significant agonist or antagonist effects, with AC50 values greater than 30000.0 nM in most assays..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest. |
| Targets&IC50 | PDE3:1.1 μM |
| Synonyms | Piteranometozine, OPC-8212, Arkin |
| Molecular Weight | 395.45 |
| Formula | C22H25N3O4 |
| Cas No. | 81840-15-5 |
| Smiles | COc1ccc(cc1OC)C(=O)N1CCN(CC1)c1ccc2NC(=O)CCc2c1 |
| Relative Density. | 1.246g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.96 mg/mL (10.01 mM), Sonication is recommended.  | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.53 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Calculator
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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