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Purity: ≥98%
Enoximone is a novel and selective phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM and with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. Enoximone prevents the degradation of cAMP by PDE, which prolongs signal transduction and its subsequent effects. It is used in patients with congestive heart failure.
| 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].
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| 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].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Bioavailabvility is 50% following oral administration. Metabolism / Metabolites Hepatic oxidation Biological Half-Life 4-10 hours |
| Toxicity/Toxicokinetics |
Protein Binding
85% |
| References |
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| Additional Infomation |
Enoximone is an aromatic ketone.
Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Trials were halted in the U.S., but the drug is used in various countries. A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE. Drug Indication For the treatment of congestive heart failure. Mechanism of Action Further research is required to determine accurately the mechanism of action of drugs with phosphodiesterase inhibitory activity, however, inhibition of PDE3 inhibits degredation of cGMP. This allows for increased NO release and vascular relaxation. Pharmacodynamics Enoximone is a phosphodiesterase inhibitor (type III) that increases the force of contraction of the heart and dilates blood vessels. In June 2005, Myogen announced that they were discontinuing development of enoximone due to negative results. The drug is approved for use in the UK. |
| 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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