LY2955303-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELY2955303Cat.No.:HY-107765CASNo.:1433497-19-8分⼦式:C₃₆H₄₂N₄O₃分⼦量:578.74作⽤靶点:RAR/RXR;Autophagy作⽤通路:MetabolicEnzyme/Protease;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:30mg/mL(51.84mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7279mL8.6395mL17.2789mL5mM0.3456mL1.7279mL3.4558mL10mM0.1728mL0.8639mL1.7279mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(3.46mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2mg/mL(3.46mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LY2955303⼀种有效且有选择性的视酸受体γ(RARγ)的拮抗剂，其Ki值为1.09nM。IC50&TargetKi:1.09nM(RARγ)[1]体外研究LY2955303istestedandobservedthatthebindingKisforRARα,RARβandRARγare>1700,>2980and1.09nM,respectively.ThefunctionalKiforRARγis7.1±4.9nM[1].体内研究AsingleoraldoseofLY2955303demonstratesadoseresponsiveeffectwherebytheratreducesdifferentialweightbearing(ED50=0.72mg/kg)[1].户使⽤本产品发表的科研⽂献•CellRes.2022Jun;32(6):513-529.•MediatorsInflamm.2022Nov7;2022:1875736.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HughesNE,etal.Identificationofpotentandselectiveretinoicacidreceptorgamma(RARγ)antagonistsforthetreatmentofosteoarthritispainusingstructurebaseddrugdesign.BioorgMedChemLett.2016Jul15;26(14):3274-3277.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8