Alprostadil (Synonyms: Prostaglandin E1, PGE1;Prostaglandin E1) |
| カタログ番号GC17347 |
アルプロスタジル (Alprostadil) はプロスタノイド受容体リガンドであり、Kis はそれぞれマウス EP3、EP4、EP2、IP、および EP1 に対して 1.1 nM、2.1 nM、10 nM、33 nM、および 36 nM です。
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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.
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