SR1001-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESR1001Cat.No.:HY-13421CASNo.:1335106-03-0分?式:C??H??F?N?O?S?分?量:477.4作?靶點(diǎn):ROR作?通路:MetabolicEnzyme/Protease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:≥39mg/mL(81.69mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0947mL10.4734mL20.9468mL5mM0.4189mL2.0947mL4.1894mL10mM0.2095mL1.0473mL2.0947mL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)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.36mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.36mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.36mM);ClearsolutionBIOLOGICALACTIVITY?物活性SR1001選擇性的RORα和RORγt反向激動(dòng)劑，Ki分別為172和111nM。體外研究SR1001inhibitsthedevelopmentofmurineTH17cellsbyinhibitionofIL-17Ageneexpressionandproteinproduction.SR1001reducestheinteractionofacoactivatorTRAP220NRbox2peptidewithRORγinadosedependentmanner(IC50value≈117nM).Additionally,SR1001inhibitstheexpressionofcytokineswhenaddedtodifferentiatedmurineorhumanTH17cells[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JNeuroinflammation.2022Jul14;19(1):186.?JNutrBiochem.24September2022,109155.?FASEBJ.2019Apr;33(4):5704-5715.?IntImmunopharmacol.2022May7;109:108778.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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