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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 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.

Enoximone 化学结构 CAS号:77671-31-9
Enoximone 化学结构
CAS号:77671-31-9
Enoximone 3D分子结构
CAS号:77671-31-9
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]}
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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。

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

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
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