Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDLin-KC2-DMACat.No.:HY-112758CASNo.:1190197-97-7分?式:C??H??NO?分?量:642.09作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:-20°C,storedundernitrogen*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(155.74mM;Needultrasonic)Ethanol:100mg/mL(155.74mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.5574mL7.7871mL15.5741mL5mM0.3115mL1.5574mL3.1148mL10mM0.1557mL0.7787mL1.5574mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(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?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.89mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.89mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.89mM);ClearsolutionBIOLOGICALACTIVITY?物活性DLin-KC2-DMA?種可電離陽(yáng)離?脂質(zhì)(pKa≈6)，對(duì)抗原呈遞細(xì)胞(APCs)?乎?毒性。DLin-KC2-DMA與納?脂質(zhì)顆粒(LNP)結(jié)合后，可產(chǎn)?明顯的siRNA介導(dǎo)的GAPDH因沉默。DLin-KC2-DMA可?于siRNA傳遞的研究。體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemEResult:SignificantlyreducedGAPDHproductioninperitonealcavitymacrophagesanddendriticcellsandinthespleen-derivedAPCswhenat5mg/kg.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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