SR1001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESR1001Cat.No.:HY-13421CASNo.:1335106-03-0分⼦式:C₁₅H₁₃F₆N₃O₄S₂分⼦量:477.4作⽤靶点:ROR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:≥39mg/mL(81.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0947mL10.4734mL20.9468mL5mM0.4189mL2.0947mL4.1894mL10mM0.2095mL1.0473mL2.0947mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.36mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.36mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.36mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SR1001选择性的RORα和RORγt反向激动剂，Ki分别为172和111nM。体外研究SR1001inhibitsthedevelopmentofmurineTH17cellsbyinhibitionofIL-17Ageneexpressionandproteinproduction.SR1001reducestheinteractionofacoactivatorTRAP220NRbox2peptidewithRORγinadosedependentmanner(IC50value≈117nM).Additionally,SR1001inhibitstheexpressionofcytokineswhenaddedtodifferentiatedmurineorhumanTH17cells[1].体内研究SR1001effectivelysuppressestheclinicalseverityofautoimmunediseaseinmice.AdministrationofSR1001toC57BL/6micesuppressestheexpressionofhepaticRORtargetgenes,Cyp7b1,Rev-erbα,andSerpine1[1].SR1001aRORαinverseagonisteliminatsthecircadianpatternofexpressionofcitratesynthasemRNAinmice[2].PROTOCOLCellAssay[1]HEK293cellsareplatedin96-wellplatesatadensityof15x103cells/well.TransfectionsareperformedusingLipofectamine2000.24hpost-transfection,thecellsaretreatedwithvehicleorcompound(SR1001).24hpost-treatment,theluciferaseactivityismeasuredusingtheDual-Gloluciferaseassaysystem[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:ExperimentalautoimmuneencephalomyelitisisinducedinC57BL/6wild-typemicebys.c.injectionAdministration[1]overfoursitesintheflankwith200μgpermouse.TheSR1001isdissolvedinDMSOat25mg/mLandthemicearetreated(i.p.)with25mg/kgSR1001(1μL/gbodyweightofmouse)orvehicle(DMSO,1μL/gbodyweightofmouse)twiceperday.Thetreatmentisstarted2daysbeforeimmunizationandcontinueduntiltheendofexperiment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JNeuroinflammation.2022Jul14;19(1):186.•JNutrBiochem.24September2022,109155.•FASEBJ.2019Apr;33(4):5704-5715.•IntImmunopharmacol.2022May7;109:108778.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].SoltLA,etal.SuppressionofTH17differentiationandautoimmunitybyasyntheticRORligand.Nature.2011Apr28;472(7344):491-4.[2].CrumbleyC,etal.Regulationofexpressionofcitratesynthasebytheretinoicacidreceptor-relatedorphanreceptorα(RORα).PLoSOne.2012;7(4):e33804.McePdfHeightCaution:Productha