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Enoximone
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Enoximone图片
CAS NO:77671-31-9

烯氟酮
Enoximone 是一种正性肌力血管舒张剂,也是一种选择性的,具有口服活性的磷酸二酯酶 III (PDE3) 抑制剂,IC50为 5.9 μM。Enoximone 通过抑制 cGMP 抑制的 PDE 来诱导血管舒张并增加细胞内 cAMP 水平。Enoximone 还表现出PDE4抑制作用,对心肌PDE4AIC50为 21.1 μM。Enoximone 可用于充血性心力衰竭的研究,并具有支气管扩张,抗哮喘和抗炎作用。
生物活性

Enoximone is an inotropic vasodilating agent and a selective and orally activephosphodiesteraseIII (PDE3)inhibitor with anIC50of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibitsPDE4inhibitory effect with anIC50of 21.1 μM formyocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects[1][2][3].

IC50& Target[1]

PDE3/PDE Ⅲ

5.9 μM (IC50)

PDE4A

21.1 μM (IC50, myocardial PDE4A)

体外研究
(In Vitro)

In vitro, 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[1].

体内研究
(In Vivo)

Topical Enoximone (25 μg; intratracheal route) abrogates house dust mite (HDM)-induced allergic airway inflammation[1].
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].

Clinical Trial
分子量

248.30

性状

Solid

Formula

C12H12N2O2S

CAS 号

77671-31-9

中文名称

烯氟酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0274 mL20.1369 mL40.2739 mL
5 mM0.8055 mL4.0274 mL8.0548 mL
10 mM0.4027 mL2.0137 mL4.0274 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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