Terlipressin Acetate

Names

[ Name ]:
Terlipressin Acetate

[Synonym ]:
(2S)-1-{[(4R,7S,10S,13S,16S,19R)-19-{[({[(Aminoacetyl)amino]acetyl}amino)acetyl]amino}-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-(4-hydroxybenzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl]carbonyl}-N-{(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxo-2-hexanyl}-2-pyrrolidinecarboxamide acetate (1:2)

Biological Activity

[Description]:

Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controlling acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock treatment[1][2][3][4][5].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor

Research Areas >> Inflammation/Immunology

[Target]

Vasopressin V1 receptor[1]

[In Vitro]

Terlipressin (25 nM; 24-72 hours; IEC-6 cells) treatment significantly improves cell viability, proliferation and apoptosis in IEC-6 cells[1]. Terlipressin inhibits the secretion of TNF-α and 15-F2t-isoprostane from IEC-6 cells following oxygen and glucose deprivation/re-oxygenation (OGD/R). Terlipressin administration following OGD attenuates OGD/R-induced cell damage via the PI3K signaling pathway[1]. Cell Proliferation Assay[1] Cell Line: IEC-6 cells induced by oxygen and glucose deprivation/re-oxygenation (OGD/R) Concentration: 25 nM Incubation Time: 24 hours, 48 hours, 72 hours Result: Significantly increased the proliferation of IEC-6 cells.

[In Vivo]

Using a mouse nonlethal hepatic ischemia-reperfusion (IR) model, Terlipressin administration significantly ameliorates IR-induced liver apoptosis, necrosis and inflammation[3].

[References]

[1]. Zi-Meng Liu, et al. Terlipressin Protects Intestinal Epithelial Cells Against Oxygen-Glucose Deprivation/Re-Oxygenation Injury via the Phosphatidylinositol 3-kinase Pathway. Exp Ther Med. 2017 Jul;14(1):260-266.

[2]. Yeun Tarl Fresner Ng Jao, et al. Refractory Torsade De Pointes Induced by Terlipressin (Glypressin). Int J Cardiol. 2016 Nov 1;222:135-140.

[3]. Xiqiang Liu, et al. Signaling Through Hepatocyte Vasopressin Receptor 1 Protects Mouse Liver From Ischemia-Reperfusion Injury. Oncotarget. 2016 Oct 25;7(43):69276-69290.

[4]. Xinmiao Zhou, et al. Terlipressin for the Treatment of Acute Variceal Bleeding: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Medicine (Baltimore). 2018 Nov;97(48):e13437.

[5]. Alastair O'Brien, et al. Terlipressin for Norepinephrine-Resistant Septic Shock. Lancet. 2002 Apr 6;359(9313):1209-10.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₂H₇₄N₁₆O₁₅S_2.xC₂H₄O₂

[ Molecular Weight ]:
1347.476

[ Exact Mass ]:
1346.538330

[ Storage condition ]:
-20°C

Related Compounds

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