DLin-KC2-DMA-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDLin-KC2-DMACat.No.:HY-112758CASNo.:1190197-97-7分⼦式:C₄₃H₇₉NO₂分⼦量:642.09作⽤靶点:Others作⽤通路:Others储存⽅式:-20°C,storedundernitrogen*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:100mg/mL(155.74mM;Needultrasonic)Ethanol:100mg/mL(155.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5574mL7.7871mL15.5741mL5mM0.3115mL1.5574mL3.1148mL10mM0.1557mL0.7787mL1.5574mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.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%salineSolubility:≥2.5mg/mL(3.89mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.89mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.89mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DLin-KC2-DMA⼀种可电离阳离⼦脂质(pKa≈6)，对抗原呈递细胞(APCs)⼏乎⽆毒性。DLin-KC2-DMA与纳⽶脂质颗粒(LNP)结合后，可产⽣明显的siRNA介导的GAPDH因沉默。DLin-KC2-DMA可⽤于siRNA传递的研究。体外研究DLin-KC2-DMA(1,5μg;72h)effectivelyproducesasignificantsiRNA-mediatedGAPDHgenesilencinginbothmacrophagesanddendriticcells[1].DLin-KC2-DMA(24h)exhibitshighuptakeintomacrophagesanddendriticcells[1].DLin-KC2-DMAefficientlypromotesreleaseofencapsulatedsiRNAintothecytosolfollowinguptakeviatheendocytoticpathway[1].DLin-KC2-DMAdisplaysalmostnotoxicityinprimaryAPCs[1].CellCytotoxicityAssay[1]CellLine:Macrophages,dendriticcellsConcentration:5μg/mL(DLin-KC2-DMAcontained-LNPs)IncubationTime:72hResult:Displayedalmostnotoxicity.WesternBlotAnalysis[1]CellLine:Macrophages,dendriticcellsConcentration:1,5μgIncubationTime:72hResult:ExhibitedsignificantGAPDHsilencingofmorethan60%at1μgandof80%at5μginmacrophages.SignificantlyreducedGAPDHproteinandexhibitedthesilencingeffectsof83%at5μg.体内研究DLin-KC2-DMAcontained-LNPsiRNAsystems(5mg/kg;i.v.;single)effectivelysilencestargetgenesinAPcsinvivo[1].AnimalModel:NaiveC57BL/6mice[1].Dosage:3or5mg/kg(DLin-KC2-DMAcontained-LNPs)Administration:Intravenousinjection;single.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:SignificantlyreducedGAPDHproductioninperitonealcavitymacrophagesanddendriticcellsandinthespleen-derivedAPCswhenat5mg/kg.户使⽤本产品发表的科研⽂献•AnalChem.2022Jun14.•bioRxiv.September30,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BashaG,etal.InfluenceofcationiclipidcompositionongenesilencingpropertiesoflipidnanoparticleformulationsofsiRNAinantigen-presentingcells.MolTher.2011Dec;19(12):2186-200.[2].MillerAD,etal.DeliveryofRNAitherapeutics:workinprogress.ExpertRevMedDevices.2013Nov;10(6):781-811.McePdfHeightCaution:Producthasnotbeenfullyvalidated