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Prostaglandin E2

现货
Catalog No.
B7005
内源性前列腺素
组合的产品项目
规格价格库存 数量
5mg
¥ 670.00
现货
10mg
¥ 950.00
现货
50mg
¥ 4,280.00
现货

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Background

Ki = 9.1, 4.9, 0.33, 0.79 nM for EP1, EP2, EP3, and EP4 receptors respectively [1]

Prostaglandin E2 (PGE2) is lipid-derived autacoid which is the main effector prostanoid produced in the zebrafish, and it works by binding and activating the PGE2 receptor. PGE2 receptor is a orphan G protein-coupled receptor.

In vitro: PGE2 can stimulate the gastric nonparietal secretion [3] and has been shown to regulate the function of many cell types including dendritic cells, macrophages, T and B lymphocytes leading to both pro- and anti-inflammatory effects [2].

In vivo: PGE2 regulates many physiological systems including the gastrointestinal and immune systems. In the gastrointestinal tract, PGE2 plays a protective role in maintaining the integrity of the gastric mucosa. PGE2 has also been shown to play a role in the maintenance of blood pressure, particularly in the setting of salt overload [2].

Clinical trial: PGE2 has cytoprotective properties, which prevents mucosal damage of the gastrointestinal tract and also accelerates the healing of existent duodenal ulcers [3]. PGE2 is the active ingredient of dinoprostone, which is a medicine used in labour for softening the cervix and causing uterine contraction.

References:
[1] Abramovitz M1, Adam M, Boie Y, Carrière M, Denis D, Godbout C, Lamontagne S, Rochette C, Sawyer N, Tremblay NM, Belley M, Gallant M, Dufresne C, Gareau Y, Ruel R, Juteau H, Labelle M, Ouimet N, Metters KM.  The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93.
[2] Hata AN, Breyer RM.  Pharmacology and signaling of prostaglandin receptors: multiple roles in inflammation and immune modulation. Pharmacol Ther. 2004 Aug;103(2):147-66.
[3] Johansson C, Kollberg B.  Clinical trials with prostaglandin E2. Prostaglandins. 1981;21 Suppl:161-4.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt352.47
Cas No.363-24-6
FormulaC20H32O5
Solubility≥35.2mg/mL in Ethanol
Chemical Name(Z)-7-((1R,2R,3R)-3-hydroxy-2-((S,E)-3-hydroxyoct-1-en-1-yl)-5-oxocyclopentyl)hept-5-enoic acid
SDFDownload SDF
Canonical SMILESO[C@H](C1)[C@H](/C=C/[C@H](CCCCC)O)[C@@H](C/C=C\CCCC(O)=O)C1=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HEK293细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

N/A

应用

在HEK293细胞中,prostaglandin E2结合FP受体,Ki值为119nM。肾脏中PGE2的产生对于正常肾功能是至关重要的,通过在生理压力下保留肾血流量和肾小球滤过率,调节远端小管中的盐和水运输以及刺激肾小球肾脏的肾素释放来保证正常的肾功能。

临床试验[2]:

疾病模型

风湿病患者

剂量

口服,1 mg,每日3次或0.33 mg,每日3次

应用

在患有风湿性疾病的患者中,吲哚美辛引起的出血通过伴随口服PGE2(1 mg,每日三次)可降低至对照水平,在口服PGE2 0.33 mg,每日三次时也显著降低出血。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Hata AN, Breyer RM. Pharmacology and signaling of prostaglandin receptors: multiple roles in inflammation and immune modulation. Pharmacol Ther. 2004 Aug;103(2):147-66.

[2] Johansson C, Kollberg B. Clinical trials with prostaglandin E2. Prostaglandins. 1981;21 Suppl:161-4.

质量控制

化学结构

Prostaglandin E2