Enoximone
Enoximone structure
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Common Name | Enoximone | ||
|---|---|---|---|---|
| CAS Number | 77671-31-9 | Molecular Weight | 248.301 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C12H12N2O2S | Melting Point | 255-258°C | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of EnoximoneEnoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects[1][2][3]. |
| Name | 4-methyl-5-(4-methylsulfanylbenzoyl)-1,3-dihydroimidazol-2-one |
|---|---|
| Synonym | More Synonyms |
| Description | Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects[1][2][3]. |
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| Related Catalog | |
| Target |
PDE3/PDE Ⅲ:5.9 μM (IC50) PDE4A:21.1 μM (IC50, myocardial PDE4A) |
| In Vitro | 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[1]. |
| In Vivo | Topical Enoximone (25 μg; intratracheal route) abrogates house dust mite (HDM)-induced allergic airway inflammation[1]. 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[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Melting Point | 255-258°C |
| Molecular Formula | C12H12N2O2S |
| Molecular Weight | 248.301 |
| Exact Mass | 248.061951 |
| PSA | 91.02000 |
| LogP | 3.72 |
| Appearance of Characters | solid | light yellow |
| Index of Refraction | 1.645 |
| InChIKey | ZJKNESGOIKRXQY-UHFFFAOYSA-N |
| SMILES | CSc1ccc(C(=O)c2[nH]c(=O)[nH]c2C)cc1 |
| Storage condition | Store at +4°C |
| Water Solubility | DMSO: 28 mg/mL, soluble |
| Personal Protective Equipment | Eyeshields;Gloves;half-mask respirator (US);multi-purpose combination respirator cartridge (US) |
|---|---|
| RIDADR | 3249 |
| WGK Germany | 3 |
| Packaging Group | III |
| Hazard Class | 6.1(b) |
| HS Code | 2933290090 |
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Enoximone CAS#:77671-31-9 |
| Literature: US4405635 A1, ; |
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Enoximone CAS#:77671-31-9 |
| Literature: Schnettler; Dage; Grisar Journal of Medicinal Chemistry, 1982 , vol. 25, # 12 p. 1477 - 1481 |
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Enoximone CAS#:77671-31-9 |
| Literature: Arkivoc, , vol. 2014, # 2 p. 294 - 307 |
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Enoximone CAS#:77671-31-9 |
| Literature: Arkivoc, , vol. 2014, # 2 p. 294 - 307 |
| HS Code | 2933290090 |
|---|---|
| Summary | 2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Recovery of heart function in children with acute severe heart failure.
Transplantation 85(7) , 975-9, (2008) The prognosis of acute heart failure is such that many children are considered for transplantation. Recovery of severe heart failure in a proportion of patients diagnosed with either dilated cardiomyo... |
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Effects of enoximone on peripheral and central chemoreflex responses in humans.
Am. J. Physiol. Heart Circ. Physiol. 294(1) , H322-9, (2008) cAMP plays an important role in peripheral chemoreflex function in animals. We tested the hypothesis that the phosphodiesterase inhibitor and inotropic medication enoximone increases peripheral chemor... |
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[Tolerance of enoximone in patients with heart failure].
Z. Kardiol. 80 Suppl 4 , 93-7, (1991) Enoximone, a new phosphodiesterase-inhibitor with positive inotropic and vasodilating activities is available for intravenous use in patients with severe heart failure. A review of the current knowled... |
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Name: Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay
Source: ChEMBL
Target: N/A
External Id: CHEMBL1266185
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Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
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Name: Fluorescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: muscarinic acetylcholine receptor M1 [Homo sapiens]
External Id: CHRM1_AG_FLUO8_1536_1X%ACT PRUN
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Name: Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: lu...
Source: 824
External Id: CYP273
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Name: Fluorescence-based cell-based primary high throughput screening assay to identify pos...
Source: The Scripps Research Institute Molecular Screening Center
Target: muscarinic acetylcholine receptor M1 [Homo sapiens]
External Id: CHRM1_PAM_FLUO8_1536_1X%ACT PRUN
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Name: Equieffective dose for contractility in anesthetized dogs for a maximum dose of 3.0 m...
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL668547
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Name: qHTS Assay for Small Molecule Inhibitors of the Human hERG Channel Activity
Source: NCGC
External Id: HERG01
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Name: Peak percent change in contractile force produced by the administration of 1 mg/kg in...
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL663786
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Name: qHTS for Inhibitors of TGF-b: Cytotox Counterscreen
Source: NCGC
Target: N/A
External Id: SMAD3201
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| Fenoximone |
| Enoximonum [Latin] |
| 5-methyl-4-(4-(methylthio)benzoyl)-1H-imidazol-2(3H)-one |
| [14C]-Enoximone |
| 4-Methyl-5-[4-(methylsulfanyl)benzoyl]-1,3-dihydro-2H-imidazol-2-one |
| Enoximona |
| MFCD00867130 |
| Perfane |
| Enoximonum |
| Enoximona [Spanish] |
| 1,3-dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one |
| Enoximone |
| Perfan |