GSK805-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK805Cat.No.:HY-12776CASNo.:1426802-50-7分?式:C??H??Cl?F?NO?S分?量:532.36作?靶點:ROR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:≥100mg/mL(187.84mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8784mL9.3921mL18.7843mL5mM0.3757mL1.8784mL3.7569mL10mM0.1878mL0.9392mL1.8784mL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(fù)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(dāng)?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(dāng)保存；體內(nèi)實驗的?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:≥2.5mg/mL(4.70mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK805?種具有?服活性和中樞神經(jīng)系統(tǒng)可透性的RORγt抑制劑。GSK805抑制RORγ和Th17細(xì)胞分化，其pIC50為8.4和>8.2。GSK805抑制Th17細(xì)胞的功能。GSK805可?于免疫的研究。IC50&TargetIC50:8.4(RORγt)[1]體外研究GSK805(0.5μM;4d)inhibitsTh17cellresponses[2].CellDifferentiationAssay[2]CellLine:CD4+TcellsConcentration:0.5μMIncubationTime:4daysResult:InhibitedIL-17productionduringTh17celldifferentiation.體內(nèi)研究GSK805(10mg/kg;p.o.onceperdayfor35days)improvesthesituationofmicewithexperimentalautoimmuneencephalomyelitis(EAE)[2].GSK805(30mg/kg;p.o.once)inhibitsTh17cellresponsesinEAEmice[2].AnimalModel:C57BL/6micewereimmunizedwithMOG35–55plusCFA[2]Dosage:10mg/kgAdministration:Oralgavage;10mg/kgonceperday;for35daysResult:EfficientlyamelioratedtheseverityofEAEinmice.AnimalModel:C57BL/6micewithEAE[2]Dosage:30mg/kgAdministration:Oralgavage;30mg/kgonceResult:ReducedbothIFN-γ-IL-17+andIFN-γ+IL-17+TcellswithoutalteredthefrequencyofTNF-α+TcellsinEAEmice.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?NatMicrobiol.2019Mar;4(3):492-503.?ProcNatlAcadSciUSA.2021Nov16;118(46):e2105950118.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].XiaoS,etal.Small-moleculeRORγtantagonistsinhibitThelper17celltranscriptionalnetworkbydivergentmechanisms.Immunity.2014Apr17;40(4):477-89.[2].WangY,etal.DiscoveryofBiarylAmidesasPotent,OrallyBioavailable,andCNSPenetrantRORγtInhibitors.ACSMedChemLett.2015May26;6(7):787-792.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic