特利加壓素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetTerlipressinCat. No.: HY-12554CAS No.: 14636-12-5分式: CHNOS分量: 1227.37Sequence: Gly-Gly-Gly-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Lys-Gly-NH2 (Disulfide bridge: Cys4-Cys9)Sequence Shortening: GGGCYFQNCPKG-NH2 (Disulfide bridge: Cys4-Cys9)作靶點: Vasopressin Receptor作通路: GPCR/G Protein儲存式: Please

2、 store the product under the recommended conditions in the COA.溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (81.48 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 0.8148 mL 4.0738 mL 8.1475 mL5 mM 0.1630 mL 0.8148 mL 1.6295 mL10 mM 0.0815 mL 0.4074 mL 0.8148 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分

3、裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PE

4、G300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.04 mM); Clear solution此案可獲得 2.5 mg/mL (2.04 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.0

5、4 mM); Clear solution此案可獲得 2.5 mg/mL (2.04 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.04 mM); Clear solution此案可獲得 2.5 mg/mL (2.04 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1

6、mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Terlipressin 種具有有效管活性特性的加壓素類似物，也 種度選擇性的加壓素 V1 受體激動劑，可減少內(nèi) 臟流量和門脈壓并控制急性靜脈曲張破裂出。Terlipressin 具有抗炎和抗氧化作，可于肝腎綜合征和耐去甲腎上腺素的敗性休克的研究。IC & Target Vasopressin V1 receptor1體外研究 Terlipressin (25 nM; 24-72 hours; IEC-6 cells) treatment

7、significantly improves cell viability, proliferation and apoptosisin IEC-6 cells1.Terlipressin inhibits the secretion of TNF- and 15-F2t-isoprostane from IEC-6 cells following oxygen and glucosedeprivation/re-oxygenation (OGD/R). Terlipressin administration following OGD attenuates OGD/R-induced cel

8、ldamage via the PI3K signaling pathway1.Cell Proliferation Assay1Cell Line: IEC-6 cells induced by oxygen and glucose deprivation/re-oxygenation (OGD/R)Concentration: 25 nMIncubation Time: 24 hours, 48 hours, 72 hoursResult: Significantly increased the proliferation of IEC-6 cells.體內(nèi)研究 Using a mouse

9、 nonlethal hepatic ischemia-reperfusion (IR) model, Terlipressin administration significantly amelioratesIR-induced liver apoptosis, necrosis and inflammation3.REFERENCES1. Zi-Meng Liu, et al. Terlipressin Protects Intestinal Epithelial Cells Against Oxygen-Glucose Deprivation/Re-Oxygenation Injury

10、via the Phosphatidylinositol3-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

11、Protects Mouse Liver From Ischemia-Reperfusion Injury. Oncotarget. 2016 Oct25;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 OBrien, et al. Terlipressin for Norepinephrine-Resistant Septic Shock. Lancet. 2002 Apr 6;359(9313):1209-10.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully va