Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPeretinoinCat.No.:HY-100008CASNo.:81485-25-8Synonyms:NIK333分?式:C??H??O?分?量:302.45作?靶點(diǎn):RAR/RXR;SphK;Autophagy;HCV作?通路:MetabolicEnzyme/Protease;Immunology/Inflammation;Autophagy;Anti-infection儲(chǔ)存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(165.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.3063mL16.5317mL33.0633mL5mM0.6613mL3.3063mL6.6127mL10mM0.3306mL1.6532mL3.3063mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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(8.27mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.27mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.27mM);ClearsolutionBIOLOGICALACTIVITY?物活性Peretinoin?種?服?環(huán)狀類視醇，具有類維?素A結(jié)構(gòu)，靶向類視醇核受體，例如RXR和RAR。Peretinoin通過下調(diào)轉(zhuǎn)錄因?Sp1，在體外降低SPHK1的mRNA?平。Peretinoin通過增加Atg16L1表達(dá)激活?噬途徑，防??精性脂性肝炎(NASH)和肝細(xì)胞癌(HCC)的發(fā)展。Peretinoin通過改變脂質(zhì)代謝來抑制HCVRNA擴(kuò)增和病毒釋放，EC50為9μM。體外研究Peretinoin(5?μM;24?hours)up-regulatestheexpressionofLC3B-IIandincreasesautophagyfluxinmouseprimaryhepatocytes[2].Peretinoin(10-40?μM;12-72?hours)exhibitssuppressedSPHK1expressionafter24?htreatment,evenat10?μMandmoreprominentafter72hperetinointreatment[1].CellAutophagyAssay[2]CellLine:Mouseprimaryhepatocytes(MPH)andthehumanHCCHepG2celllineConcentration:5?μMIncubationTime:24hoursResult:Up-regulatedtheexpressionofLC3B-IIandincreasedautophagyflux.WesternBlotAnalysis[1]CellLine:Humanhepatoma(Huh-7)cellsConcentration:10,20and40?μMIncubationTime:12,24,48and72?hoursResult:ExhibitedsuppressedSPHK1expressionafter24?htreatment,evenat10?μM.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ArteriosclerThrombVascBiol.2020Mar;40(3):656-669.?AntiviralRes.2019Oct;170:104570.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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