2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Vesnarinone

Vesnarinone  (Synonyms: OPC-8212)

Cat. No.: HY-15297 Purity: 98.58%
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Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research.

For research use only. We do not sell to patients.

Vesnarinone Chemical Structure

Vesnarinone Chemical Structure

CAS No. : 81840-15-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Vesnarinone Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Vesnarinone

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research[1][2][3][4].

In Vitro

Vesnarinone (60 and 100 μg/mL; 48 h) inhibits the cell growth in a dose-dependent manner[3].
Vesnarinone (60 μg/mL; 48 h) induces G1 arrest and apoptosis[3].
Vesnarinone (60 μg/mL; 0, 12, 24, and 48 h) treatment increases p21-mRNA expression and decreases p21 protein slightly[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Vesnarinone Related Antibodies

Cell Viability Assay[3]

Cell Line: OSC3, OSC4, and OSC5 cells
Concentration: 60 μg/mL and 100 μg/mL
Incubation Time: 48 hours
Result: Observed more than 50% inhibition in cells treated with 100 μg/mL, and reduced 30±40% the production of MTT formazan in cells treated with 60 μg/mL.

Apoptosis Analysis[3]

Cell Line: OSC3, OSC4, and OSC5 cells
Concentration: 60 μg/mL
Incubation Time: 48 hours
Result: Decreased the tumor cell population in the S phase and increased in the G1 phase.

Western Blot Analysis[3]

Cell Line: OSC3, OSC4, and OSC5 cells
Concentration: 60 μg/mL
Incubation Time: 0, 12, 24, and 48 hours
Result: Increased the expression of p21-mRNA after 12±24 h vesnarinone treatment.
Decreased p21 protein slightly after 24 h treatment in OSC4.
In Vivo

Vesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver in vivo[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats (200 g)[4]
Dosage: 300 mg/kg
Administration: Oral gavage; 300 mg/kg; once daily; 6 weeks
Result: Observed covalently modified liver proteins.
Clinical Trial
Molecular Weight

395.45

Formula

C22H25N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(C=C(N3CCN(C(C4=CC=C(OC)C(OC)=C4)=O)CC3)C=C2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (42.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5288 mL 12.6438 mL 25.2876 mL
5 mM 0.5058 mL 2.5288 mL 5.0575 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (4.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (4.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5288 mL 12.6438 mL 25.2876 mL 63.2191 mL
5 mM 0.5058 mL 2.5288 mL 5.0575 mL 12.6438 mL
10 mM 0.2529 mL 1.2644 mL 2.5288 mL 6.3219 mL
15 mM 0.1686 mL 0.8429 mL 1.6858 mL 4.2146 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1610 mL
25 mM 0.1012 mL 0.5058 mL 1.0115 mL 2.5288 mL
30 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5805 mL
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Vesnarinone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vesnarinone81840-15-5OPC-8212OPC8212OPC 8212Phosphodiesterase (PDE)oral activityphosphodiesterase 3positive inotropic activityheart failureOSC3OSC4OSC5Inhibitorinhibitorinhibit

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