E1231-1-4-2-5-Methylfuran-2-yl-quinoline-4-carbonyl-piperazin-1-yl-ethan-1-one-DataSheet-生命科學(xué)試劑-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:C??H??N?O?分子量:363.41作用靶點(diǎn):Sirtuin作用通路:CellCycle/DNADamage;Epigenetics儲(chǔ)存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(275.17mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7517mL13.7586mL27.5171mL5mM0.5503mL2.7517mL5.5034mL10mM0.2752mL1.3759mL2.7517mL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；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存方式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨?。以下溶解方案都?qǐng)先按照InVitro方式配制澄清的儲(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，澄清的儲(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)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶)1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.88mM);Clearsolution請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.88mM);ClearsolutionBIOLOGICALACTIVITY生物活性 E1231是一種具有口服有效的Sirtuin1(SIRT1)(EC50=0.83μM)激活劑，可調(diào)節(jié)膽固醇和脂質(zhì)代謝。E1231與SIRT1和脫乙酰肝X受體-α(LXRα)相互作用，并增加ATP結(jié)合盒轉(zhuǎn)運(yùn)蛋白A1(ABCA1)的表達(dá)。E1231還可以減少ApoE-/-小鼠模型中動(dòng)脈粥樣硬化斑塊的形成。E1231可用于膽固醇和脂質(zhì)紊亂相關(guān)疾病的研究。IC50&TargetSIRT10.83μM(EC50)體外研究E1231(0.1-10μM;18h)promotescholesteroleffluxandinhibitslipidaccumulationinRAW264.7cells[1].E1231(10μM;6h)significantlyincreasesdeacetylationofDoxo-inducedp53inHepG2cells[1].體內(nèi)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—您身邊的抑制劑大師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic