Olitigaltin-TD139-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOlitigaltinCat.No.:HY-19940CASNo.:1450824-22-2Synonyms:TD139;GB0139分⼦式:C₂₈H₃₀F₂N₆O₈S分⼦量:648.64作⽤靶点:Galectin作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(77.08mM;Needultrasonic)Ethanol:≥3.33mg/mL(5.13mM)H2O:≥1mg/mL(1.54mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5417mL7.7084mL15.4169mL5mM0.3083mL1.5417mL3.0834mL10mM0.1542mL0.7708mL1.5417mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE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(3.85mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.85mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.85mM);Clearsolution4.请依序添加每种溶剂：10%HP-β-CDSolubility:3.33mg/mL(5.13mM);Clearsolution;Needultrasonic5.请依序添加每种溶剂：15%CremophorEL>>85%SalineSolubility:2mg/mL(3.08mM);Clearsolution;Needultrasonic6.请依序添加每种溶剂：45%PEG300>>5%Tween-80>>50%salineSolubility:10mg/mL(15.42mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性TD139吸⼊式的半乳凝素-3(galectin-3)抑制剂，Kd值为14nM。IC50&TargetKd:14nM(galectin-3)[1]体外研究TD139isanovelsyntheticinhibitorofgalectin-3.TD139hashighaffinityforgalectin-3withaKdof14nMand10nMforgalectin-1,butlowaffinityforgalectins2,4N,4C,7,8N,or9N[1].体内研究InprimarylungAECsTD139reducesTGF-β1–inducedβ-catenintranslocationtothenucleus,withmostoftheβ-cateninremainingatthecellsurface.TD139blocksTGF-β1–inducedβ-cateninphosphorylation.Amarkedreductioninfibrosisandβ-cateninactivationaccompaniedbydecreasedgalectin-3expressionisobservedinthelungsofWTmicetreatedwithTD139[1].PretreatmentofWTC57BL/6micewithTD139leadstotheattenuationofliverinjuryandmilderinfiltrationofIFNγ-andIL-17-and-4-producingCD4(+)Tcells,aswellasanincreaseinthetotalnumberofIL-10-producingCD4(+)TcellsandF4/80(+)CD206(+)alternativelyactivatesmacrophagesandpreventestheapoptosisofliver-infiltratingMNCs[2].PROTOCOLAnimalMice:ThesusceptibilitytoConA-inducedhepatitisingalectin-3-deficientmiceistestedandtheeffectsofAdministration[2]pretreatmentwithaselectiveinhibitorofGal-3(TD139)inwild-type(WT)C57BL/6miceareanalyzed,asevaluatedbyaliverenzymetest,quantitativehistology,mononuclearcell(MNC)infiltration,cytokineproduction,intracellularstainingofimmunecells,andpercentageofapoptoticMNCsintheliver[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Autophagy.2021Oct6;1-29.•JNeuroinflammation.17September2022.•StemCellResTher.2021Jul16;12(1):409.•ExpNeurol.2023Apr19;114418.•ChemBiolInteract.9October2022,110218.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MackinnonAC,etal.Regulationoftransforminggrowthfactor-β1-drivenlungfibrosisbygalectin-3.AmJRespirCritCareMed.2012Mar1;185(5):537-46.[2].VolarevicV,etal.Galectin-3deficiencypreventsconcanavalinA-inducedhepatitisinmice.Hepatology.2012Jun;55(6):1954-64.McePdfHeightCaution: