Enoximone|77671-31-9|(烯氟酮)-陌孚医药/Medlife

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Enoximone (Synonyms: 烯氟酮)

目录号: PC12647 纯度: ≥98%

CAS No. :77671-31-9

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中文名称

Enoximone

中文别名

依诺昔酮;1,3-二氢-4-甲基-5-(4-甲基硫代苯甲酰)-2H-咪唑-2-酮;1,3-二氢-4-甲基-5-(4-甲硫基苯甲酰基)-2H-咪唑-2-酮;氢甲苯咪酮

英文名称

Enoximone

英文别名

Enoximone;1,3-Dihydro-4-methyl-5-(4-methylthiobenzoyl)-2H-imidazol-2-one;4-methyl-5-(4-methylsulfanylbenzoyl)-1,3-dihydroimidazol-2-one;[14C]-Enoximone;1,3-dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one;5-methyl-4-(4-(methylthio)benzoyl)-1H-imidazol-2(3H)-one;Enoximona;Enoximona [Spanish];Enoximonum;Enoximonum [Latin];Fenoximone;Perfan;Perfane

Cas No.

77671-31-9

分子式

C₁₂H₁₂N₂O₂S

分子量

248.30

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

IC50 & Target[1][2]

PDE3/PDE Ⅲ

5.9 μM (IC₅₀)

PDE4A

21.1 μM (IC₅₀, myocardial PDE4A)

体外研究(In Vitro)

体外研究, 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Jan Beute, et al. A Pathophysiological Role of PDE3 in Allergic Airway Inflammation. JCI Insight. 2018 Jan 25;3(2):e94888. [Information]

[2]. R C Dage, et al. Pharmacology and Pharmacokinetics of Enoximone. Cardiology. 1990;77 Suppl 3:2-13; discussion 27-33. [Information]

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

溶解度数据

体外研究:

DMSO : 8.33 mg/mL (33.55 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0274 mL	20.1369 mL	40.2739 mL
5 mM	0.8055 mL	4.0274 mL	8.0548 mL
10 mM	0.4027 mL	2.0137 mL	4.0274 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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