Vesnarinone
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.52%
- No. CAS: 81840-15-5
- Fòrmula: C22H25N3O4
- Peso molecular:395.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-15297R
Vesnarinone (Standard)PDE3 Inhibitor -
HY-90009A
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IBMXPDE Inhibitor -
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Tadalafil (Standard)PDE5 Inhibitor -
HY-16900
RolipramPDE4 Inhibitor -
HY-15455
RoflumilastPDE4 Inhibitor -
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SildenafilPDE5 Inhibitor -
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IbudilastPhosphodiesterase Inhibitor -
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HY-B0715
PentoxifyllinePDE Inhibitor
Publications Citing Use of MedChemExpress (MCE) Vesnarinone
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Actividad biológica
Descripciòn
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.
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Cell Line:OSC3, OSC4, and OSC5 cells
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Concentration:60 μg/mL and 100 μg/mL
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Incubation Time:48 hours
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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.
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Cell Line:OSC3, OSC4, and OSC5 cells
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Concentration:60 μg/mL
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Incubation Time:48 hours
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Result:Decreased the tumor cell population in the S phase and increased in the G1 phase.
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Cell Line:OSC3, OSC4, and OSC5 cells
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Concentration:60 μg/mL
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Incubation Time:0, 12, 24, and 48 hours
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rats (200 g)[4]
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Dosage:300 mg/kg
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Administration:Oral gavage; 300 mg/kg; once daily; 6 weeks
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Result:Observed covalently modified liver proteins.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 81840-15-5
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Appearance Solid
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Peso molecular 395.45
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Fòrmula C22H25N3O4
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Color White to off-white
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SMILES
O=C1NC2=C(C=C(N3CCN(C(C4=CC=C(OC)C(OC)=C4)=O)CC3)C=C2)CC1
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Synonyms
OPC-8212
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Drug Metab Dispos
An in vitro approach to predict idiosyncratic drug-induced agranulocytosis using myeloperoxidase-derived reactive metabolites. [Abstract]2026 Jun;54(6):100324. PMID: 42248123 -
Toxicol Lett
Discovery of non-steroidal aldo-keto reductase 1D1 inhibitors through automated screening and in vitro evaluation. [Abstract]2025 Apr:406:31-37. PMID: 39988211 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (397 KB)
- English - EN (397 KB)
- Français - FR (397 KB)
- Deutsch - DE (397 KB)
- Norwegian - NO (397 KB)
- Español - ES (397 KB)
- Swedish - SV (397 KB)
- Italian - IT (397 KB)
- Korean - KR (397 KB)
- Portuguese - PT (397 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. A Matsumori, et al. Vesnarinone, a new inotropic agent, inhibits cytokine production by stimulated human blood from patients with heart failure. Circulation. 1994 Mar;89(3):955-8. [Content Brief]
[2]. E Cavusoglu, et al. Vesnarinone: a new inotropic agent for treating congestive heart failure. J Card Fail. 1995 Jun;1(3):249-57. [Content Brief]
[3]. K Yoneda, et al. Induction of cyclin-dependent kinase inhibitor p21 in vesnarinone-induced differentiation of squamous cell carcinoma cells. Cancer Lett. 1998 Nov 13;133(1):35-45. [Content Brief]
[4]. Iain Gardner, et al. A comparison of the covalent binding of clozapine, procainamide, and vesnarinone to human neutrophils in vitro and rat tissues in vitro and in vivo. Chem Res Toxicol. 2005 Sep;18(9):1384-94. [Content Brief]
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 |
Vesnarinone Related Classifications
HY-15297 Related Classifications
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