Alprostadil
(Synonyms: 前列地尔; Alprostadil; PGE1;Prostaglandin E1) 目录号 : GC17347
前列地尔Alprostadil作为前列腺素受体配体,对小鼠EP3、EP4、EP2、IP和EP1的结合亲和Kis分别为1.1 nM、2.1 nM、10 nM、33 nM和36 nM。
Cas No.:745-65-3
Sample solution is provided at 25 µL, 10mM.
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Alprostadil functions as a prostanoid receptor ligand, exhibiting binding affinities Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM, and 36 nM for murine EP3, EP4, EP2, IP, and EP1, correspondingly. Alprostadil can inhibit platelet aggregation and thrombin A2 production, and has diuretic and renal function protection [1-3].
Alprostadil(0.1-50 ng/ml; 8-26h) causes an upregulation of eNOS and VEGF protein and mRNA expression in HUVEC and decreases HIF-1alpha[4]. Alprostadil (10 ng/mL; 24h) reduces apoptosis and improves the homing of mesenchymal stem cells in pulmonary arterial hypertension by regulating hypoxia-inducible factor 1 alpha[5].
Alprostadil(5 ug/kg; i.p) can reduce pancreatic tissue damage, delay pancreatic cell apoptosis, and reduce inflammation and anti-oxidative stress by inhibiting the JAK2/STAT3 signal pathway, thus protecting the pancreas in acute pancreatitis rat model[6]. Alprostadil (0.3125, 0.625, and 1.25 mg/kg/d; i.p) attenuates AngII-induced cardiac hypertrophy via E-prostanoid (EP) 3 receptor activation and Netrin-1upregulation[7].
References:
[1]. Kiriyama M, Ushikubi F, et,al. Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. doi: 10.1038/sj.bjp.0701367. PMID: 9313928; PMCID: PMC1564924.
[2]. Cattaneo MG, Pola S, et,al. Alprostadil suppresses angiogenesis in vitro and in vivo in the murine Matrigel plug assay. Br J Pharmacol. 2003 Jan;138(2):377-85. doi: 10.1038/sj.bjp.0705051. PMID: 12540529; PMCID: PMC1573673.
[3]. Hauck EW, Altinkilic BM, et,al. Prostaglandin E1 long-term self-injection programme for treatment of erectile dysfunction--a follow-up of at least 5 years. Andrologia. 1999;31 Suppl 1:99-103. doi: 10.1111/j.1439-0272.1999.tb01458.x. PMID: 10643527.
[4]. Haider DG, Bucek RA, et,al. PGE1 analog alprostadil induces VEGF and eNOS expression in endothelial cells. Am J Physiol Heart Circ Physiol. 2005 Nov;289(5):H2066-72. doi: 10.1152/ajpheart.00147.2005. Epub 2005 Jun 10. PMID: 15951350.
[5]. Jiang DT, Tuo L, et,al. Prostaglandin E1 reduces apoptosis and improves the homing of mesenchymal stem cells in pulmonary arterial hypertension by regulating hypoxia-inducible factor 1 alpha. Stem Cell Res Ther. 2022 Jul 16;13(1):316. doi: 10.1186/s13287-022-03011-x. PMID: 35842683; PMCID: PMC9288720.
[6]. Fei S, Li W, et,al. Protective Effect of Alprostadil on Acute Pancreatitis in Rats via Inhibiting Janus Kinase 2 (JAK2)/STAT3 Signal Transduction Pathway. Med Sci Monit. 2019 Oct 13;25:7694-7701. doi: 10.12659/MSM.919148. PMID: 31606729; PMCID: PMC6807527.
[7]. Shen Y, Wang X, et,al. Prostaglandin E1 attenuates AngII-induced cardiac hypertrophy via EP3 receptor activation and Netrin-1upregulation. J Mol Cell Cardiol. 2021 Oct;159:91-104. doi: 10.1016/j.yjmcc.2021.06.009. Epub 2021 Jun 18. PMID: 34147480.
前列地尔Alprostadil作为前列腺素受体配体,对小鼠EP3、EP4、EP2、IP和EP1的结合亲和Kis分别为1.1 nM、2.1 nM、10 nM、33 nM和36 nM。 Alprostadil能够抑制血小板聚集和血栓素A2生成,有利尿和保护肾功能的作用[1-3]。
Alprostadil (0.1-50 ng/ml; 8-26h)引起HUVEC中eNOS和VEGF蛋白及mRNA表达上调,降低HIF-1alpha [4]。Alprostadil (10 ng/mL; 24h)通过调节HIF-1alpha,减少肺动脉高压中细胞凋亡,促进间充质干细胞归巢[5]。
Alprostadil (5 ug/kg; i.p)可通过抑制JAK2/STAT3信号通路,减轻胰腺组织损伤,延缓胰腺细胞凋亡,减轻炎症和抗氧化应激,从而保护急性胰腺炎模型大鼠胰腺[6]。Alprostadil (0.3125, 0.625, and 1.25 mg/kg/d; i.p)通过E-prostanoid (EP) 3受体激活和Netrin -1上调来减轻血管内皮细胞诱导的心肌肥大[7]。
| Cell experiment [1]: | |
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Cell lines |
Human umbilical vein endothelial cells (HUVEC) |
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Preparation Method |
Alprostadil was incubated with HUVEC for 8 h at 0.1, 1.0, 5.0, 10.0, or 50.0 ng/ml under normoxic conditions. Cells were then exposed in the presence of alprostadil to either normoxic or hypoxic conditions (6% O2-94% N2) for an additional 12 or 18 h. |
|
Reaction Conditions |
0.1-50 ng/ml; 8-26h |
|
Applications |
Incubation with alprostadil dose-dependently upregulated mRNA expression of eNOS and VEGF under normoxia and downregulated HIF-1α expression. Exposure of HUVEC to hypoxia increased eNOS, VEGF, and HIF-1α mRNA and protein compared with normoxic conditions. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley rats (Acute Pancreatitis model) |
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Preparation Method |
Rat was intraperitoneally injected with alprostadil 5 ug/kg 30 min before AP modeling. Rats were sacrificed after 48 h. |
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Dosage form |
5 ug/kg; i.p |
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Applications |
Alprostadil could reduce oxidative stress and inhibits proinflammatory cytokine release. |
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References: [1]. Haider DG, Bucek RA, et,al. PGE1 analog alprostadil induces VEGF and eNOS expression in endothelial cells. Am J Physiol Heart Circ Physiol. 2005 Nov;289(5):H2066-72. doi: 10.1152/ajpheart.00147.2005. Epub 2005 Jun 10. PMID: 15951350. |
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| Cas No. | 745-65-3 | SDF | |
| 别名 | 前列地尔; Alprostadil; PGE1;Prostaglandin E1 | ||
| 化学名 | 7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]heptanoic acid | ||
| Canonical SMILES | CCCCCC(C=CC1C(CC(=O)C1CCCCCCC(=O)O)O)O | ||
| 分子式 | C20H34O5 | 分子量 | 354.48 |
| 溶解度 | ≥ 13.4mg/mL in DMSO | 储存条件 | Store at -20°C, stored under nitrogen,unstable in solution, ready to use. |
| 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 | 2.821 mL | 14.1052 mL | 28.2103 mL |
| 5 mM | 0.5642 mL | 2.821 mL | 5.6421 mL |
| 10 mM | 0.2821 mL | 1.4105 mL | 2.821 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。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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