Terlipressin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETerlipressinCat.No.:HY-12554CASNo.:14636-12-5分⼦式:C₅₂H₇₄N₁₆O₁₅S₂分⼦量:1227.37Sequence: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:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:100mg/mL(81.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.8148mL4.0738mL8.1475mL5mM0.1630mL0.8148mL1.6295mL10mM0.0815mL0.4074mL0.8148mL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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.04mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.04mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.04mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Terlipressin⼀种具有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。Terlipressin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].户使⽤本产品发表的科研⽂献•SciRep.2020Dec3;10(1):21037.Seemorecustomervalidationsonwww.MedChemEREFERENCES[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):69276-69290.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[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:Producthasnotbeenfully