Peretinoin-NIK333-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPeretinoinCat.No.:HY-100008CASNo.:81485-25-8Synonyms:NIK333分⼦式:C₂₀H₃₀O₂分⼦量:302.45作⽤靶点:RAR/RXR;SphK;Autophagy;HCV作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation;Autophagy;Anti-infection储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:50mg/mL(165.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3063mL16.5317mL33.0633mL5mM0.6613mL3.3063mL6.6127mL10mM0.3306mL1.6532mL3.3063mL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(protectfromlight,storedundernitrogen)。-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:≥2.5mg/mL(8.27mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.27mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.27mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Peretinoin⼀种⼝服⾮环状类视醇，具有类维⽣素A结构，靶向类视醇核受体，例如RXR和RAR。Peretinoin通过下调转录因⼦Sp1，在体外降低SPHK1的mRNA⽔平。Peretinoin通过增加Atg16L1表达激活⾃噬途径，防⽌⾮精性脂性肝炎(NASH)和肝细胞癌(HCC)的发展。Peretinoin通过改变脂质代谢来抑制HCVRNA扩增和病毒释放，EC50为9μM。体外研究Peretinoin(5ꢀμM;24ꢀhours)up-regulatestheexpressionofLC3B-IIandincreasesautophagyfluxinmouseprimaryhepatocytes[2].Peretinoin(10-40ꢀμM;12-72ꢀhours)exhibitssuppressedSPHK1expressionafter24ꢀhtreatment,evenat10ꢀμMandmoreprominentafter72hperetinointreatment[1].CellAutophagyAssay[2]CellLine:Mouseprimaryhepatocytes(MPH)andthehumanHCCHepG2celllineConcentration:5ꢀμMIncubationTime:24hoursResult:Up-regulatedtheexpressionofLC3B-IIandincreasedautophagyflux.WesternBlotAnalysis[1]CellLine:Humanhepatoma(Huh-7)cellsConcentration:10,20and40ꢀμMIncubationTime:12,24,48and72ꢀhoursResult:ExhibitedsuppressedSPHK1expressionafter24ꢀhtreatment,evenat10ꢀμM.户使⽤本产品发表的科研⽂献•ArteriosclerThrombVascBiol.2020Mar;40(3):656-669.•AntiviralRes.2019Oct;170:104570.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].FunakiM,etal.Peretinoin,anacyclicretinoid,inhibitshepatocarcinogenesisbysuppressingsphingosinekinase1expressioninvitroandinvivo.SciRep.2017Dec5;7(1):16978.[2].OkadaH,etal.Peretinoin,anacyclicretinoid,suppressessteatohepatitisandtumorigenesisbyactivatingautophagyinmicefedanatherogenichigh-fatdiet.Oncotarget.2017Jun20;8(25):39978-39993.[3].HondaM,etal.Peretinoin,anacyclicretinoid,improvesthehepaticgenesignatureofchronichepatitisCfollowingcurativetherapyofhepatocellularcarcinoma.BMCCancer.2013Apr15;13:191.McePdfHeightCaution:Producthasnotbeenfullyval