77671-31-9
Enoximone
CAS: 77671-31-9
Molecular Formula: C12H12N2O2S
77671-31-9 - Names and Identifiers
77671-31-9 - Physico-chemical Properties
| Molecular Formula | C12H12N2O2S |
| Molar Mass | 248.3 |
| Density | 1.33 |
| Melting Point | 255-258°C |
| Solubility | DMSO: 28 mg/mL, soluble |
| Appearance | Form solid, color light yellow |
| pKa | 10.37±0.70(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Physical and Chemical Properties | Chemical properties from isopropanol-water crystallization, melting point 255-258 ℃ (decomposition). |
| Use | The use of strong selective phosphodiesterase III inhibitors, strong heart and dilation of blood vessels, but rarely cause symptomatic hypotension. For acute and chronic congestive heart failure as well as cardiac surgery and heart failure complicated by low cardiac output status. |
77671-31-9 - Risk and Safety
| UN IDs | 3249 |
| WGK Germany | 3 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
77671-31-9 - Upstream Downstream Industry
| Raw Materials | Ethyl acetate NITROUS ACID |
77671-31-9 - Uses and synthesis methods
biological activity
Enoximone is a positive inotropic vasodilator and a selective, orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induce vasodilation and increase intracellular cAMP levels by inhibiting PDE inhibited by cGMP. Enoximone also showed PDE4 inhibition with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone can be used in the study of congestive heart failure and has bronchodilatation, anti-asthma and anti-inflammatory effects.
target
PDE3/PDE Ⅲ
5.9 μM (IC 50 )
PDE4A
21.1 μM (IC 50 , myocardial PDE4A)
in vitro study
In vitro, 10 μM Enoximone-treated bronchoalveolar lavage (BAL) eosinophils induced by IL-33 treatment shows significantly lower CD11b expression when compared with diluent-treated BAL eosinophils.
in vivo studies
Topical Enoximone (25 μg; intratracheal route) abrogates house dust mite (HDM)-induced allergic airway inflammation.
The Enoximone-treated (25 μg; for 5 days) HDM-exposed mice shows significant reductions in inflammatory cell numbers including eosinophils, macrophages, neutrophils, ILC2s, and T cells, indicating that Enoximone treatment reduces airway inflammation.
production method
After ethyl acetoacetate is reacted with nitrous acid, it is then catalytically hydrogenated to obtain ethyl α-amino acetoacetate, and the imidazole ring derivative is cyclized with isocyanate, and the sodium hydroxide aqueous solution is hydrolyzed and decarboxylated, and finally acylated Enoxian.
Last Update：2024-04-09 19:04:55
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CAS: 77671-31-9
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CAS: 77671-31-9
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Mobile: 18021002903
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Raw Materials for 77671-31-9