Terlipressin-acetate-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETerlipressinacetateCat.No.:HY-12554ACASNo.:1884420-36-3分⼦式:C₅₆H₈₂N₁₆O₁₉S₂分⼦量:1347.48Sequence:Gly-Gly-Gly-Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Lys-Gly-NH2(Disulfidebridge:Cys4-Cys9)SequenceShortening:GGGCYFQNCPKG-NH2(Disulfidebridge:Cys4-Cys9)作⽤靶点:VasopressinReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:100mg/mL(74.21mM;Needultrasonic)DMSO:100mg/mL(74.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.7421mL3.7106mL7.4213mL5mM0.1484mL0.7421mL1.4843mL10mM0.0742mL0.3711mL0.7421mL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，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(1.86mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(1.86mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Terlipressinacetate⼀种具有⾎管活性的加压素类似物，也⼀种⾼度选择性的加压素V1受体激动剂，可减少内脏⾎流量和门脉压⼒并控制急性静脉曲张破裂出⾎。Terlipressinacetate具有抗炎和抗氧化作⽤，可⽤于肝肾综合征和耐去甲肾上腺素的败⾎性休克的研究。IC50&TargetVasopressinV1receptor[1]体外研究Terlipressin(25nM;24-72hours;IEC-6cells)treatmentsignificantlyimprovescellviability,proliferationandapoptosisinIEC-6cells[1].TerlipressininhibitsthesecretionofTNF-αand15-F2t-isoprostanefromIEC-6cellsfollowingoxygenandglucosedeprivation/re-oxygenation(OGD/R).TerlipressinadministrationfollowingOGDattenuatesOGD/R-inducedcelldamageviathePI3Ksignalingpathway[1].CellProliferationAssay[1]CellLine:IEC-6cellsinducedbyoxygenandglucosedeprivation/re-oxygenation(OGD/R)Concentration:25nMIncubationTime:24hours,48hours,72hoursResult:SignificantlyincreasedtheproliferationofIEC-6cells.体内研究Usingamousenonlethalhepaticischemia-reperfusion(IR)model,TerlipressinadministrationsignificantlyamelioratesIR-inducedliverapoptosis,necrosisandinflammation[3].REFERENCES[1].Zi-MengLiu,etal.TerlipressinProtectsIntestinalEpithelialCellsAgainstOxygen-GlucoseDeprivation/Re-OxygenationInjuryviathePhosphatidylinositol3-kinasePathway.ExpTherMed.2017Jul;14(1):260-266.[2].YeunTarlFresnerNgJao,etal.RefractoryTorsadeDePointesInducedbyTerlipressin(Glypressin).IntJCardiol.2016Nov1;222:135-140.[3].XiqiangLiu,etal.SignalingThroughHepatocyteVasopressinReceptor1ProtectsMouseLiverFromIschemia-ReperfusionInjury.Oncotarget.2016Oct25;7(43):69276-69290.[4].XinmiaoZhou,etal.TerlipressinfortheTreatmentofAcuteVaricealBleeding:ASystematicReviewandMeta-AnalysisofRandomizedControlledTrials.Medicine(Baltimore).2018Nov;97(48):e13437.[5].AlastairO'Brien,etal.TerlipressinforNorepinephrine-ResistantSepticShock.Lancet.2002Apr6;359(9313):1209-10.McePdfHeightCaution:Producthasnotbeenfullyvalidate