Larsucosterol-trimethylamine-DUR-928-trimethylamine-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELarsucosterol(trimethylamine)Cat.No.:HY-139576BSynonyms:DUR-928(trimethylamine)分?式:C??H??O?S.?.??C?H?N分?量:509.32作?靶點(diǎn):LXR;EndogenousMetabolite作?通路:MetabolicEnzyme/Protease;VitaminDRelated/NuclearReceptor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:33.33mg/mL(65.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9634mL9.8170mL19.6340mL5mM0.3927mL1.9634mL3.9268mL10mM0.1963mL0.9817mL1.9634mL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?。BIOLOGICALACTIVITY?物活性Larsucosterol(DUR-928)trimethylamine?種膽醇代謝物，?種有效的肝X受體(LXR)拮抗劑。Larsucosteroltrimethylamine?種有效的內(nèi)性脂?成調(diào)節(jié)劑。Larsucosteroltrimethylamine通過降低mRNA?平和抑制SREBP-1的激活抑制膽醇的?物合成。1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究Larsucosterol(DUR-928;0-25μM;8h;HepG2cells)trimethylamineinhibitscholesterolbiosynthesisbydecreasingHMG-CoAreductasemRNAlevelsanddecreasesfree[14C]cholesterolinadose-dependentmanner[1].Larsucosterol(0-25μM;6h;HepG2cells)trimethylamineinhibitsHMG-CoAreductaseexpressionbyinhibitionofbothSREBP1activationandexpressioninhepatocytes[1].Larsucosterol(0-50μM;48h)trimethylamineincreasescellproliferationanddecreasesapoptosisinmacrophages[2].Larsucosterol(0-25μM;48h;macrophages)trimethylamineinhibitsactivationofliveroxysterolreceptorLXRα[2].CellProliferationAssay[2]CellLine:MacrophagesConcentration:0,5,10,15,20,and25μMIncubationTime:48hoursResult:Inducescellproliferationandrelativecellnumberaftertreatmentfor48hwere120%at25μM.ApoptosisAnalysis[2]CellLine:MacrophagesConcentration:0,10,20,30,40and50μMIncubationTime:48hoursResult:Didnotsignificantlyaffectthenumbersofapoptoticorlivecells.WesternBlotAnalysis[1]CellLine:HepG2cellsConcentration:0,3,6,12,and25μMIncubationTime:6hoursResult:InhibitedtheactivationofSREBP-1andSREBP-2,andsubsequentlyinhibittheexpressionHMG-CoAreductase.WesternBlotAnalysis[2]CellLine:MacrophagesConcentration:0,3,6,12,and25μMIncubationTime:48hours2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:DecreasedLXRαlevelsinthenucleiinadoes-dependentmanner.體內(nèi)研究Larsucosterol(DUR-928;25mg/kg;i.p.;twicein14hours;C57BL/6Jmicewithnonalcoholicfattyliverdiseases(NAFLD)model)trimethylaminereducesserumlipidlevelsinmicefedahigh-fatdiet[3].Larsucosterol(25mg/kg;i.p.;twicein14hours;C57BL/6Jmicewithnonalcoholicfattyliverdiseases(NAFLD)model)trimethylaminesuppressedtheexpressionofthegenesandinhibitsABCA1expressionde.LarsucosterolcreasesnuclearSREBP-1ProteinlevelsandcytoplasmicFASandACC1proteinlevelsinlivertissue[3].Larsucosterol(25mg/kg;i.p.;onceevery3daysfor6weeks;C57BL/6Jmicewithnonalcoholicfattyliverdiseases(NAFLD)model)trimethylamineprotectstheliverfrominjurybysuppressinghepaticinflammation[3].AnimalModel:FemaleC57BL/6Jmicewithnonalcoholicfattyliverdiseases(NAFLD)model[3]Dosage:25mg/kgAdministration:Intraperitonealinjection;twicein14hoursResult:DecreasedplasmaTG,CHOL,andHDL-Cby40,15,and20%,respectively.ReducedthemRNAlevelsofSREBP-1c,ACC1,andFASby46,57,and49%,respectively.SuppressedABCA1expression.SuppressednuclearSREBP-1,cytoplasmicACC1,andFASproteinlevelsby74,58,and47%,respectively.AnimalModel:FemaleC57BL/6Jmicewithnonalcoholicfattyliverdiseases(NAFLD)model[3]Dosage:25mg/kgAdministration:Intraperitonealinjection;onceevery3daysfor6weeksResult:Decreasedplasmacholesterollevels.Reducedserumalkalinephosphatase,ALT,andASTlevels.REFERENCES[1].RenS,et,al.Sulfatedoxysterol,25HC3S,isapotentregulatoroflipidmetabolisminhumanhepatocytes.BiochemBiophysResCommun.2007Sep7;360(4):802-8.[2].MaY,et,al.25-Hydroxycholesterol-3-sulfateregulatesmacrophagelipidmetabolismviatheLXR/SREBP-1signalingpathway.AmJPhysiolEndocrinolMetab.2008Dec;295(6):E1369-79.[3].XuL,et,al.5-cholesten-3β,25-diol3-sulfatedecreaseslipidaccumulationindiet-inducednonalcoholicfattyliverdiseasemousemodel.MolPharmacol.2013Mar;83(3):648-58.McePdfHeight3/3MasterofBioactiveMolec