ZED-1227-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZED-1227Cat.No.:HY-19359CASNo.:1542132-88-6分⼦式:C₂₆H₃₆N₆O₆分⼦量:528.6作⽤靶点:Glutaminase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(236.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8918mL9.4589mL18.9179mL5mM0.3784mL1.8918mL3.7836mL10mM0.1892mL0.9459mL1.8918mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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:2.08mg/mL(3.93mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.93mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.93mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ZED-1227⼀种特异性的，具有⼝服活性的转⾕氨酰胺酶2(TG2)抑制剂，IC50值为45nM。ZED-1227能阻塞炎症诱导的TG2表达和激活，可⽤于乳糜泻的研究[1][2]。IC50&TargetIC50:45nM(TG2)[2]体外研究ZED-1227(0.1μΜ-1μΜ;24hours)hasnoeffectonmetabolicactivityandproliferationinHuh7cellsandCaCo2cells,thatsuggestsZED-1227hasnocytotoxicactivity[2].ZED-1227(0.002-0.2mg/mL;30minutes)inhibitsTG2inthesmallintestinalmucosainvitro[2].体内研究ZED-1227reducestheactivityofintestinalTG2inducedbyPolyinosinic:Polycytidylicacid(40mg/kg)tonormalcontrollevelsandsubduesintestinalinflammationinmice[1].ZED-1227(5mg/kg;i.g.)isabletoinhibitTG2inthesmallintestinalmucosa[2].AnimalModel:BALB/cmice[2]Dosage:5mg/kgAdministration:OralgavageResult:InhibitedTG2invivointhesmallintestinalmucosa.REFERENCES[1].ManuEncalada,etal.TheOralTransglutaminase2(TG2)InhibitorZed1227BlocksTG2ActivityinaMouseModelofIntestinalInflammation.Gastroenterology.154(6):S-490.[2].ChristianBüchold,etal.Pyridinonederivativesastissuetransglutaminaseinhibitors.WO2014012858A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch