Enoximone | 烯氟酮 | MDL 17043 | PDE3 Inhibitor | AmBeed-信号通路专用抑制剂

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依诺昔酮 /Enoximone {[allProObj[0].p_purity_real_show]}

货号：A414763 同义名： 烯氟酮 / MDL 17043

Enoximone是一种正性肌力作用的血管扩张剂，选择性且口服活性的磷酸二酯酶 III 抑制剂，IC50 为 5.9 μM，具有支气管扩张、抗哮喘和抗炎作用，可用于充血性心力衰竭研究。

Enoximone 化学结构
CAS号：77671-31-9

Enoximone 3D分子结构
CAS号：77671-31-9

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Enoximone 纯度/质量文件产品仅供科研

货号：A414763 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

PDE 亚型比较

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	✔								mAChR,AChR	99%
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	99%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				99% (HPLC)
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				99% (HPLC)
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ HPDE4, IC50: 120 nM LPDE4, IC50: 100 nM				99%
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。

Enoximone 生物活性

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].

Enoximone 临床研究

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 <<

Enoximone 参考文献

[1]Beute J, Lukkes M, Koekoek EP, Nastiti H, Ganesh K, de Bruijn MJ, Hockman S, van Nimwegen M, Braunstahl GJ, Boon L, Lambrecht BN, Manganiello VC, Hendriks RW, KleinJan A. A pathophysiological role of PDE3 in allergic airway inflammation. JCI Insight. 2018 Jan 25;3(2):e94888

[2]Dage RC, Okerholm RA. Pharmacology and pharmacokinetics of enoximone. Cardiology. 1990;77 Suppl 3:2-13; discussion 27-33

[3]M B Vroom, et al. Effect of Phosphodiesterase Inhibitors on Human Arteries in Vitro. Br J Anaesth. 1996 Jan;76(1):122-9.

[4]Beute J, Boermans P, Benraad B, Telman J, Diamant Z, KleinJan A. PDE3-inhibitor enoximone prevented mechanical ventilation in patients with SARS-CoV-2 pneumonia. Exp Lung Res. 2021 Apr;47(3):149-160

[5]Lowes BD, Higginbotham M, Petrovich L, DeWood MA, Greenberg MA, Rahko PS, Dec GW, LeJemtel TH, Roden RL, Schleman MM, Robertson AD, Gorczynski RJ, Bristow MR. Low-dose enoximone improves exercise capacity in chronic heart failure. Enoximone Study Group. J Am Coll Cardiol. 2000 Aug;36(2):501-8

Enoximone 实验方案

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

Enoximone 技术信息

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

In solvent -20°C:3-6个月-80°C:12个月

Pure form 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

临床研究

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 <<
NCT00060840	Congestive Heart Failure	Phase 2	Completed	-	United States, New Jersey ... 展开 >> Newark Beth Isreal Medical Center Newark, New Jersey, United States, 07112 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45219 Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 United States, Pennsylvania Allegheny General Hospital Pittsburgh, Pennsylvania, United States, 15212 United States, Texas Baylor University Medical Center Dallas, Texas, United States, 75226 University of Texas/St. Paul Medical Center Dallas, Texas, United States, 75390 Texas Heart Institute Houston, Texas, United States, 20345 Germany Herz-und Diabeteszentrum Nordrhein-Westfalen Gergstrab, Bad Oeynhausen, Germany, 32545 Deutsches Herfzzentrum Berlin Augustenburger Platz, Berlin, Germany, 13353 United Kingdom Harefield Hospital Harefield, Middlesex, United Kingdom, UB96JH 收起 <<
NCT00348101	Coronary Artery Disease	Phase 3	Completed	-	Germany ... 展开 >> Department of Anesthesiology and Intensive Care Medicine Klinikum Ludwigshafen Ludwigshafen, Germany, 67063 收起 <<
NCT02285309	-		Unknown	-	-
NCT00051285	Heart Failure, Congestive	Phase 3	Terminated	-	-
NCT03729011	Delirium	Phase 4	Not yet recruiting	January 29, 2022	-
NCT00077948	Heart Failure, Congestive	Phase 3	Terminated	-	United States, Colorado ... 展开 >> University of Colorado Denver, Colorado, United States, 80262 United States, Utah University of Utah Salt Lake City, Utah, United States, 84132 收起 <<
NCT00060840	-		Completed	-	-

依诺昔酮 /Enoximone {[allProObj[0].p_purity_real_show]}

Enoximone 纯度/质量文件产品仅供科研

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Enoximone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Enoximone 质控信息

Enoximone 生物活性

Enoximone 临床研究

Enoximone 参考文献

Enoximone 实验方案

Enoximone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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