产品说明书

Enoximone

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Chemical Structure| 77671-31-9 同义名 : 烯氟酮 ;MDL 17043
CAS号 : 77671-31-9
货号 : A414763
分子式 : C12H12N2O2S
纯度 : 98%+
分子量 : 248.301
MDL号 : MFCD00867130
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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:
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].
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 <<
实验方案
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

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