ZED-1227-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZED-1227Cat.No.:HY-19359CASNo.:1542132-88-6分?式:C??H??N?O?分?量:528.6作?靶點:Glutaminase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(236.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8918mL9.4589mL18.9179mL5mM0.3784mL1.8918mL3.7836mL10mM0.1892mL0.9459mL1.8918mL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，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C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?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(3.93mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.93mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性ZED-1227?種特異性的，具有?服活性的轉(zhuǎn)?氨酰胺酶2(TG2)抑制劑，IC50值為45nM。ZED-1227能阻塞炎癥誘導的TG2表達和激活，可?于乳糜瀉的研究[1][2]。IC50&TargetIC50:45nM(TG2)[2]體外研究ZED-1227(0.1μΜ-1μΜ;24hours)hasnoeffectonmetabolicactivityandproliferationinHuh7cellsandCaCo2cells,thatsuggestsZED-1227hasnocytotoxicactivity[2].ZED-1227(0.002-0.2mg/mL;30minutes)inhibitsTG2inthesmallintestinalmucosainvitro[2].體內(nèi)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