E1231-1-4-2-5-Methylfuran-2-yl-quinoline-4-carbonyl-piperazin-1-yl-ethan-1-one-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEE1231Cat.No.:HY-117006CASNo.:1031195-19-3Synonyms:1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one分子式:C₂₁H₂₁N₃O₃分子量:363.41作用靶点:Sirtuin作用通路:CellCycle/DNADamage;Epigenetics储存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(275.17mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制备储备液1mM2.7517mL13.7586mL27.5171mL5mM0.5503mL2.7517mL5.5034mL10mM0.2752mL1.3759mL2.7517mL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方式配制澄清的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄清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是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)1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.88mM);Clearsolution请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.88mM);ClearsolutionBIOLOGICALACTIVITY生物活性 E1231是一种具有口服有效的Sirtuin1(SIRT1)(EC50=0.83μM)激活剂，可调节胆固醇和脂质代谢。E1231与SIRT1和脱乙酰肝X受体-α(LXRα)相互作用，并增加ATP结合盒转运蛋白A1(ABCA1)的表达。E1231还可以减少ApoE-/-小鼠模型中动脉粥样硬化斑块的形成。E1231可用于胆固醇和脂质紊乱相关疾病的研究。IC50&TargetSIRT10.83μM(EC50)体外研究E1231(0.1-10μM;18h)promotescholesteroleffluxandinhibitslipidaccumulationinRAW264.7cells[1].E1231(10μM;6h)significantlyincreasesdeacetylationofDoxo-inducedp53inHepG2cells[1].体内研究E1231(40mg/kg;po;oncedailyfor7days)regulatescholesterolandlipidmetabolisminGoldenhamstersfedwithHFDdiet[1].E1231(25,50,and100mg/kg,in0.5%CMC-Na;po;oncedailyfor12weeks)reducesatherosclerosisdevelopment,withouthepatotoxicityornephrotoxicityinApoE-/-micefedwithatherogenicdiet[1].AnimalModel:HFD-dietGoldenhamsters(80-90g)[1]Dosage:40mg/kgAdministration:PO;oncedailyfor7daysResult:IncreasedSIRT1proteinexpressionbutnotSIRT3,SIRT6,orSIRT7.Andreducedliverandserumcholesterolinhamsters.AnimalModel:AtherogenicdietApoE-/-mice[1]Dosage:25,50,and100mg/kgAdministration:PO;oncedailyfor12weeksResult:Modulatedplaquecomposition,immunofluorescencestaining.AndreducedCD68positiveareaswhileincreasingABCA1expressionintheaorticsinus.REFERENCESFengT,etal.SIRT1activatorE1231protectsfromexperimentalatherosclerosisandlowersplasmacholesterolandtriglyceridesbyenhancingABCA1expression.Atherosclerosis.2018Jul;274:172-181.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic