CBR-470-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECBR-470-1Cat.No.:HY-134205ACASNo.:2416095-06-0分⼦式:C₁₄H₂₀ClNO₄S₂分⼦量:365.9作⽤靶点:Keap1-Nrf2作⽤通路:NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:200mg/mL(546.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7330mL13.6649mL27.3299mL5mM0.5466mL2.7330mL5.4660mL10mM0.2733mL1.3665mL2.7330mL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:≥5mg/mL(13.66mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(13.66mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(13.66mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CBR-470-1糖酵解磷酸⽢油酸激酶1(PGK1)的抑制剂。CBR-470-1也⼀种⾮共价的Nrf2激活剂。CBR-470-1通过激活Keap1-Nrf2级联反应，保护SH-SY5Y神经元细胞免受MPP+诱导的细胞毒性。IC50&TargetKeap1-Nrf2[2]体外研究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