Prostaglandin E2
(Synonyms: 前列腺素 E2; PGE2; Dinoprostone) 目录号 : GC15948
Prostaglandin E2是花生四烯酸在环氧合酶(COX)催化下产生的主要代谢物。
Cas No.:363-24-6
Sample solution is provided at 25 µL, 10mM.
Prostaglandin E2 is a major metabolite produced from arachidonic acid catalyzed by Cyclooxygenase (COX).It is also one of the most biologically active and widely studied prostaglandins. As a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation. [4]
Mouse bone marrow derived naïve macrophages produce prostaglandin E2 endogenously, resulting in anti-inflammatory gene expression upon differentiation induced by macrophage colony stimulating factor (M-CSF)[1]. Prostaglandin E2 has a mediator role for multiple inflammatory responses. Prostaglandin E2 receptors EP1, EP2, EP3 and EP4, are involved in the regulation of prostaglandin E2-related processes, of which[5,6], EP2 and EP4 are closely associated with inflammatio. EP2 and EP4 are involved in cytokine expression in E. coli-infected bovine endometrial tissue[7]. The affinity of PGE2 to these receptors varies according to the subtype and tissue type of the receptor, and the affinity constant (Kd) of prostaglandin E2 is about 1-10 nM. Prostaglandin E2 caused maximum relaxation of endothelin-1 precontracted vessels (EC50: 1.8×10-8M) [9].Prostaglandin E2-mediated enhancement of SPA expression in S. aureus-infected bovine endometrial tissue is dependent on EP4 receptor[4].PROSTAGLANDIN E2 induced the expression of some genes associated with alternative—M(IL-4)—cell activation including Arg1, Il4ra, and Clec10a (CD301), prostaglandin E2 accentuated IL-4-induced expression of Arg1, IL4ra, Clec10a, CD36, and Mrc1 when both stimuli where used simultaneously (co-stimulation), although it suppressed the expression of Retnla and Pparg, prostaglandin E2 did not alter IL-4-induced phosphorylation of STAT6. Thus, prostaglandin E2 has marked STAT6-independent effects on M(IL-4) cell activation[3].
The effect of intra-aortic administration of prostaglandin E2 on renal blood flow was studied in the rat anaesthetized with pentobarbitone. Dose-response curves demonstrate that under the conditions used, PROSTAGLANDIN E2 produced a biphasic change in renal vascular resistance, vasodilatation started at 0.01 μg/min and was maximal at about 3 μg/min, while at the highest dose used (20μg/min) prostaglandin E2 induced renal vasoconstriction[2].In addition, prostaglandin E2 have been shown to have complex effects on skeletal tissues, but a major effect in vivo is to increase both bone formation and bone resorption or bone remodeling, In a study in rats continuous infusion of prostaglandin E2 produced net bone loss while daily injection led to net bone gain[8].
References:
[1]: Na YR, Jung D, et,al. Endogenous prostaglandin E2 potentiates anti-inflammatory phenotype of macrophage through the CREB-C/EBP-β cascade. Eur J Immunol. 2015 Sep;45(9):2661-71. doi: 10.1002/eji.201545471. Epub 2015 Jul 20. PMID: 26118414.
[2]: Haylor J, Towers J. Renal vasodilator activity of prostaglandin E2 in the rat anaesthetized with pentobarbitone. Br J Pharmacol. 1982 May;76(1):131-7. doi: 10.1111/j.1476-5381.1982.tb09198.x. PMID: 6952954; PMCID: PMC2068751.
[3]: Sanin DE, Matsushita M, et,al. Mitochondrial Membrane Potential Regulates Nuclear Gene Expression in Macrophages Exposed to Prostaglandin E2. Immunity. 2018 Dec 18;49(6):1021-1033.e6. doi: 10.1016/j.immuni.2018.10.011. PMID: 30566880; PMCID: PMC7271981.
[4]: Liu K, Mao W, et,al. Prostaglandin E2 promotes Staphylococcus aureus infection via EP4 receptor in bovine endometrium. Microb Pathog. 2021 Sep;158:105019. doi: 10.1016/j.micpath.2021.105019. Epub 2021 Jun 6. PMID: 34107344.
[5]: Wu J, Liu B, et,al. Prostaglandin E2 Regulates Activation of Mouse Peritoneal Macrophages by Staphylococcus aureus through Toll-Like Receptor 2, Toll-Like Receptor 4, and NLRP3 Inflammasome Signaling. J Innate Immun. 2020;12(2):154-169. doi: 10.1159/000499604. Epub 2019 May 29. PMID: 31141808; PMCID: PMC7098297.
[6]: Li T, Liu B, et,al. PGE2 increases inflammatory damage in Escherichia coli-infected bovine endometrial tissue in vitro via the EP4-PKA signaling pathway. Biol Reprod. 2019 Jan 1;100(1):175-186. doi: 10.1093/biolre/ioy162. PMID: 30010723.
[7]: Zhang C, Wang L, et,al. EP2/4 Receptors Promote the Synthesis of PGE2 Increasing Tissue Damage in Bovine Endometrial Explants Induced by Escherichia coli. J Pharmacol Exp Ther. 2020 Feb;372(2):175-184. doi: 10.1124/jpet.119.262444. Epub 2019 Nov 15. PMID: 31732699.
[8]: Tian XY, Zhang Q, et,al. Continuous PGE2 leads to net bone loss while intermittent PGE2 leads to net bone gain in lumbar vertebral bodies of adult female rats. Bone. 2008 May;42(5):914-20. doi: 10.1016/j.bone.2007.12.228. Epub 2008 Feb 5. PMID: 18316259.
[9]:Astin M, Stjernschantz J. Mechanism of prostaglandin E2-, F2alpha- and latanoprost acid-induced relaxation of submental veins. Eur J Pharmacol. 1997 Dec 11;340(2-3):195-201. doi: 10.1016/s0014-2999(97)01414-3. PMID: 9537815.
| Cell experiment [1]: | |
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Cell lines |
Mouse bone-marrow-derived macrophages (BMMs) |
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Preparation Method |
BMMs were stimulated in complete RPMI supplemented with CSF-1 for indicated times with a combination of 20 ng/mL IL-4 , 10 μM prostaglandin E2, 100 μM 8-Br-cAMP, 20 μM Forskolin, 50 ng/mL IFN-γ, 20 ng/mL LPS, 100 μM Ap5a, 1.5 μM flurorcarbonyl cyanide phenylhydrazon, 10 nM valinomycin, 10 μM EdU, 10 μM KT5720, 10 μM H-89 or 2 μM α-amanitin under 5% CO2, atmospheric oxygen, at 37°C in a humidified incubator. |
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Reaction Conditions |
6h,10μM, 37°C |
|
Applications |
Prostaglandin E2 induced the expression of some genes associated with alternative—M(IL-4)—cell activation including Arg1, Il4ra, and Clec10a (CD301), prostaglandin E2 accentuated IL-4-induced expression of Arg1, IL4ra, Clec10a, CD36, and Mrc1 when both stimuli where used simultaneously (co-stimulation), although it suppressed the expression of Retnla and Pparg, prostaglandin E2 did not alter IL-4-induced phosphorylation of STAT6. Thus, prostaglandin E2 has marked STAT6-independent effects on M(IL-4) cell activation. |
| Animal experiment [2]: | |
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Animal models |
Male Wistar rats (370-430 g) |
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Preparation Method |
Prostaglandin E2 was dissolved in heparin/saline (50 units/ml) and infused via the aortic cannula in a cumulative manner in doses ranging from 0.01-20 ug/min. Each dose was infused for a 5 min period. |
|
Dosage form |
0.01ug/min-20ug/min, Prostaglandin E2 was dissolved in heparin/saline (50 units/ml) |
|
Applications |
Dose-response curves demonstrate that under the conditions used, prostaglandin E2 produced a biphasic change in renal vascular resistance, vasodilatation started at 0.01 μg/min and was maximal at about 3 μg/min, while at the highest dose used (20μg/min) prostaglandin E2 induced renal vasoconstriction. |
|
References: [1]. Sanin DE, Matsushita M, et,al. Mitochondrial Membrane Potential Regulates Nuclear Gene Expression in Macrophages Exposed to Prostaglandin E2. Immunity. 2018 Dec 18;49(6):1021-1033.e6. doi: 10.1016/j.immuni.2018.10.011. PMID: 30566880; PMCID: PMC7271981. [2]. Haylor J, Towers J. Renal vasodilator activity of prostaglandin E2 in the rat anaesthetized with pentobarbitone. Br J Pharmacol. 1982 May;76(1):131-7. doi: 10.1111/j.1476-5381.1982.tb09198.x. PMID: 6952954; PMCID: PMC2068751. |
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| Cas No. | 363-24-6 | SDF | |
| 别名 | 前列腺素 E2; PGE2; Dinoprostone | ||
| 化学名 | (Z)-7-((1R,2R,3R)-3-hydroxy-2-((S,E)-3-hydroxyoct-1-en-1-yl)-5-oxocyclopentyl)hept-5-enoic acid | ||
| Canonical SMILES | O[C@H](C1)[C@H](/C=C/[C@H](CCCCC)O)[C@@H](C/C=C\CCCC(O)=O)C1=O | ||
| 分子式 | C20H32O5 | 分子量 | 352.47 |
| 溶解度 | 70 mg/mL (198.60 mM) in DMSO, 70 mg/mL (198.60 mM) in Ethanol | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8371 mL | 14.1856 mL | 28.3712 mL |
| 5 mM | 0.5674 mL | 2.8371 mL | 5.6742 mL |
| 10 mM | 0.2837 mL | 1.4186 mL | 2.8371 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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