CBR-470-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECBR-470-1Cat.No.:HY-134205ACASNo.:2416095-06-0分?式:C??H??ClNO?S?分?量:365.9作?靶點:Keap1-Nrf2作?通路:NF-κB儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(546.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7330mL13.6649mL27.3299mL5mM0.5466mL2.7330mL5.4660mL10mM0.2733mL1.3665mL2.7330mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(13.66mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(13.66mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(13.66mM);ClearsolutionBIOLOGICALACTIVITY?物活性CBR-470-1糖酵解磷酸?油酸激酶1(PGK1)的抑制劑。CBR-470-1也?種?共價的Nrf2激活劑。CBR-470-1通過激活Keap1-Nrf2級聯(lián)反應(yīng)，保護SH-SY5Y神經(jīng)元細胞免受MPP+誘導(dǎo)的細胞毒性。IC50&TargetKeap1-Nrf2[2]體外研究CBR-470-1(0.01-10μM;24h)hasanEC50of962nMinARE-LUCreporterassayofIMR32cells[1].CBR-470-1(0.5-20μM;1-24h)resultsinadose-andtime-dependentaccumulationofNrf2proteininIMR32cells[1].CBR-470-1(10μM;4h)activatesNrf2signalingcascadeinSH-SY5Ycells[2].CBR-470-1(10μM;2h)inhibitsMPP+-inducedoxidativeinjuryinSH-SY5Yneuronalcells[2].WesternBlotAnalysis[1]CellLine:IMR32cellsConcentration:0.5,1,5,10,20μMIncubationTime:1,2,4,8,24hResult:IncreasedtheNrf2proteininadose-andtime-dependentmanner.IncreasedbothmRNAandproteinlevelsoftheNrf2-responsivegenesNQO1andHMOX1.REFERENCES[1].BollongMJ,et,al.Ametabolite-derivedproteinmodificationintegratesglycolysiswithKEAP1-NRF2signalling.Nature.2018Oct;562(7728):600-604.[2].ZhengJ,et,al.PGK1inhibitorCBR-470-1protectsneuronalcellsfromMPP+.Aging(AlbanyNY).2020Jul10;12(13):13388-13399.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu