Olitigaltin-TD139-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOlitigaltinCat.No.:HY-19940CASNo.:1450824-22-2Synonyms:TD139;GB0139分?式:C??H??F?N?O?S分?量:648.64作?靶點(diǎn):Galectin作?通路:Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(77.08mM;Needultrasonic)Ethanol:≥3.33mg/mL(5.13mM)H2O:≥1mg/mL(1.54mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.5417mL7.7084mL15.4169mL5mM0.3083mL1.5417mL3.0834mL10mM0.1542mL0.7708mL1.5417mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.85mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.85mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.85mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%HP-β-CDSolubility:3.33mg/mL(5.13mM);Clearsolution;Needultrasonic5.請(qǐng)依序添加每種溶劑：15%CremophorEL>>85%SalineSolubility:2mg/mL(3.08mM);Clearsolution;Needultrasonic6.請(qǐng)依序添加每種溶劑：45%PEG300>>5%Tween-80>>50%salineSolubility:10mg/mL(15.42mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性TD139吸?式的半乳凝素-3(galectin-3)抑制劑，Kd值為14nM。IC50&TargetKd:14nM(galectin-3)[1]體外研究TD139isanovelsyntheticinhibitorofgalectin-3.TD139hashighaffinityforgalectin-3withaKdof14nMand10nMforgalectin-1,butlowaffinityforgalectins2,4N,4C,7,8N,or9N[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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: