货号:A414763 同义名: 烯氟酮 / MDL 17043
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.
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产品名称 | PDE ↓ ↑ | PDE1 ↓ ↑ | PDE10A ↓ ↑ | PDE2 ↓ ↑ | PDE3 ↓ ↑ | PDE4 ↓ ↑ | PDE5 ↓ ↑ | PDE6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Doxofylline | ✔ | 99+% | |||||||||||||||||
Deltarasin |
+++
PDEδ , Kd: 38 nM |
99+% | |||||||||||||||||
7-(2,3-Dihydroxypropyl)theophylline | ✔ | 98% | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
98+% | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | AChR,mAChR | 98% | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 98% | |||||||||||||||||
Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
PF-2545920 |
++++
PDE10A, IC50: 0.37 nM |
97% | |||||||||||||||||
Luteolin |
+
PDE1, Ki: 15.0 μM |
++
PDE2, Ki: 6.4 μM |
+
PDE3, Ki: 13.9 μM |
+
PDE4, Ki: 11.1 μM |
+
PDE5, Ki: 9.5 μM |
98% | |||||||||||||
Milrinone |
++
PDE2, IC50: 5.2 μM |
++
PDE3, IC50: 2.1 μM |
ATPase | 98% | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
98% | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
98% | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
98% | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
HPDE4, IC50: 120 nM LPDE4, IC50: 100 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
98% | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
98% | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | 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. 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[1]. Enoximone sulphoxide has the same inotropic and vasodilator activities as enoximone but is 0.13-0.14 times as potent and has a 13 times longer duration of inotropic action in the dog[2]. Early intervention with the selective PDE3-inhibitor enoximone may help to revert respiratory failure as well as avert mechanical ventilation, and reduces ICU/hospital time in patients with severe SARS-CoV-2 pneumonia[4]. Twelve weeks of treatment with low-dose enoximone improves exercise capacity in patients with CHF(chronic heart failure), without increasing adverse events[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03772990 | Cardiac Surgery ... 展开 >> Cardiopulmonary Bypass 收起 << | Phase 4 | Not yet recruiting | March 30, 2022 | - |
NCT01864252 | Myocardial Reperfusion Injury | Phase 3 | Unknown | February 2016 | United Kingdom ... 展开 >> The Heart Hospital, UCL Hospitals NHS Trust Recruiting London, United Kingdom, NW1 2PG Contact: Ashraf Hamarneh, MBchB,MRCP 02034479781 a.hamarneh@ucl.ac.uk Principal Investigator: Derek M Yellon, PhD DSc FACC Principal Investigator: Derek J Hausenloy, MD PhD FRCP Sub-Investigator: Ashraf Hamarneh, MBchB MRCP Sub-Investigator: Shyam Kolvekar, MS MCh FRCS Sub-Investigator: Roger Cordery, BSc FRCA Sub-Investigator: Vivek Sivaraman, MRCP MD FRCA 收起 << |
NCT00484133 | Severe Sepsis ... 展开 >> Microcirculation 收起 << | Phase 4 | Unknown | - | Netherlands ... 展开 >> Onze Lieve Vrouwe Gasthuis, intensive care Recruiting Amsterdam, Netherlands, 1090 HM Contact: Rutger v Raalte, MD 0031205993007 R.vanRaalte@olvg.nl Principal Investigator: Rutger v Raalte, MD 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.03mL 0.81mL 0.40mL |
20.14mL 4.03mL 2.01mL |
40.27mL 8.05mL 4.03mL |
CAS号 | 77671-31-9 |
分子式 | C12H12N2O2S |
分子量 | 248.301 |
别名 | 烯氟酮 ;MDL 17043 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 7 mg/mL(28.19 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |