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Purity: ≥98%
| Targets |
The primary target of enoximone is phosphodiesterase III (PDE3), an enzyme that hydrolyzes cyclic AMP (cAMP) and cyclic GMP (cGMP) in cardiac and vascular smooth muscle cells. By inhibiting PDE3, enoximone increases intracellular cAMP levels, leading to enhanced calcium influx and increased contractility in cardiac myocytes (positive inotropic effect). In vascular smooth muscle cells, the increase in cAMP promotes vasodilation. Enoximone has an IC50 of 5.9 µM for PDE3 inhibition.
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| ln Vitro |
In vitro, bronchoalveolar lavage (BAL) eosinophils treated with 10 μM enoxamone generated by IL-33 exhibited notably reduced expression of CD11b in contrast to BAL eosinophils treated with diluent [1].
In vitro, enoximone is a selective PDE3 inhibitor with an IC50 of 5.9 µM. It increases intracellular cAMP levels in cardiac myocytes and vascular smooth muscle cells, leading to enhanced contractility and vasodilation. Its activity is characterized by its ability to inhibit PDE3-mediated cAMP hydrolysis. Enoximone also has bronchodilatory, antiasthma, and anti-inflammatory effects, which may be related to its PDE3 inhibitory activity in airway smooth muscle and immune cells. |
| ln Vivo |
The house dust mite (HDM)-induced allergic airway inflammation is eliminated by topical Enoximone (25 μg; intratracheal route) [1]. Enoximone administration (25 μg) for 5 days significantly decreased the number of inflammatory cells (eosinophils, neutrophils, macrophages, ILC2s, and T cells) in HDM-exposed mice, suggesting that the drug attenuates gastrointestinal tract illness. irritation of the tract[1].
In vivo, enoximone is used for the treatment of congestive heart failure. It improves cardiac function by increasing cardiac contractility (inotropic effect) and reducing afterload through vasodilation. The compound is administered intravenously for acute heart failure management and orally for chronic heart failure. Its bronchodilatory effects may be beneficial in patients with concomitant pulmonary disease. Clinical studies have demonstrated its efficacy in improving hemodynamic parameters in heart failure patients. |
| Enzyme Assay |
The in vitro activity of enoximone is assessed using cell-free PDE3 enzyme activity assays. PDE3 enzyme is incubated with a cAMP or cGMP substrate in the presence of varying concentrations of enoximone. The hydrolysis of the substrate is measured, typically using a radioactive or fluorescence-based detection method. The IC50 is determined from dose-response curves. For selectivity profiling, the compound is tested against other PDE isoforms (PDE1, PDE2, PDE4, PDE5) to assess its selectivity for PDE3.
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| Cell Assay |
For cellular assays, cardiac myocytes or vascular smooth muscle cells are cultured in appropriate media. Cells are treated with various concentrations of enoximone (typically 0.1-100 µM) for defined periods. Intracellular cAMP levels are measured by ELISA. The contractility of cardiac myocytes can be assessed by measuring cell shortening or calcium transients. The vasodilatory effect can be assessed using isolated blood vessel preparations or by measuring endothelial cell nitric oxide production. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, enoximone is typically administered intravenously or orally to patients or animal models. In animal models of heart failure, the compound is administered at various doses, and hemodynamic parameters (blood pressure, cardiac output, left ventricular pressure) are monitored. In clinical studies, the compound's efficacy is assessed by measuring improvements in exercise capacity, hemodynamic parameters, and quality of life. Pharmacokinetic studies involve measurement of enoximone plasma concentrations by HPLC or LC-MS/MS.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The bioavailability after oral administration is 50%. Metabolism/Metabolites Hepatic Oxidation Biological Half-Life 4-10 hours Enoximone has a molecular weight of 248.30 g/mol and a molecular formula of C12H12N2O2S. It is soluble in DMSO at >10 mM. The compound should be stored at +4°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's oral bioavailability makes it suitable for chronic oral administration. |
| Toxicity/Toxicokinetics |
Protein Binding
85% Enoximone can cause side effects including hypotension, headache, nausea, and arrhythmias due to its vasodilatory and positive inotropic effects. The compound should be used with caution in patients with hypotension, arrhythmias, or severe aortic stenosis. Its use in heart failure is guided by careful hemodynamic monitoring. Comprehensive toxicological studies are required to establish its full safety profile. The compound is intended for use under appropriate medical supervision. |
| References |
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| Additional Infomation |
Enoxidone is an aromatic ketone. Enoxidone is a selective phosphodiesterase inhibitor with vasodilatory and positive inotropic effects that does not alter myocardial oxygen consumption. It is used to treat patients with congestive heart failure. Clinical trials of this drug in the United States have been discontinued, but it is still used in several other countries. A selective phosphodiesterase inhibitor with vasodilatory and positive inotropic effects that does not alter myocardial oxygen consumption. It is used to treat patients with congestive heart failure. Drug Indications For the treatment of congestive heart failure. Mechanism of Action Further research is needed to determine the exact mechanism of action of drugs with phosphodiesterase inhibitory activity, but PDE3 inhibitors inhibit the degradation of cGMP. This helps increase the release of nitric oxide (NO) and dilate blood vessels. Pharmacodynamics Enoxidone is a type III phosphodiesterase inhibitor that enhances cardiac contractility and dilates blood vessels. In June 2005, Myogen announced that it had discontinued development of enoxiedon due to unsatisfactory trial results. The drug had been approved for use in the UK.
Enoximone is a clinically approved medication for the treatment of congestive heart failure in some regions. It is a selective PDE3 inhibitor that improves cardiac function through its inotropic and vasodilatory effects. Enoximone is available as an intravenous formulation for acute heart failure management and as an oral formulation for chronic heart failure. Its development represents an advance in the pharmacotherapy of heart failure, providing an alternative to other inotropic agents. It is not widely used in all regions and has been superseded by other heart failure therapies in some guidelines. |
| Molecular Formula |
C12H12N2O2S
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| Molecular Weight |
248.3
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| Exact Mass |
248.061
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| CAS # |
77671-31-9
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| Related CAS # |
77671-31-9;
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| PubChem CID |
53708
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
255-258°C
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| Index of Refraction |
1.645
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| LogP |
3.72
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
371
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZJKNESGOIKRXQY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N2O2S/c1-7-10(14-12(16)13-7)11(15)8-3-5-9(17-2)6-4-8/h3-6H,1-2H3,(H2,13,14,16) SMILES
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| Chemical Name |
4-methyl-5-(4-methylsulfanylbenzoyl)-1,3-dihydroimidazol-2-one
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| Synonyms |
EnoximonumPerfan Fenoximone MDL-17043 MDL 19438 MDL-17,043 MDL-17043 MDL-19,438 MDL17,043 MDL17043 MDL19,438 Myogen Brand of Enoximone Perfan
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8.33 mg/mL (~33.55 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0274 mL | 20.1369 mL | 40.2739 mL | |
| 5 mM | 0.8055 mL | 4.0274 mL | 8.0548 mL | |
| 10 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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