NE-52-QQ57-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENE52-QQ57Cat.No.:HY-101784CASNo.:1401728-56-0分⼦式:C₂₄H₂₈N₆O分⼦量:416.52作⽤靶点:GPR4作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:20mg/mL(48.02mM;ultrasonicandwarmingandadjustpHto5withHClandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4008mL12.0042mL24.0085mL5mM0.4802mL2.4008mL4.8017mL10mM0.2401mL1.2004mL2.4008mL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:≥2mg/mL(4.80mM);Clearsolution1/3MasterofBioactiveMolecules—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:≥2mg/mL(4.80mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2mg/mL(4.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NE52-QQ57选择性，有⼝服活性的GPR4拮抗剂，IC50为70nM[1]。NE52-QQ57具有抗炎活性[1]。IC50&TargetIC50:70nM(GPR4)[1].体外研究NE52-QQ57effectivelyblocksGPR4-mediatedcAMPaccumulation(IC5026.8ꢀnMinHEK293ꢀcells)[2].体内研究NE52-QQ57(Compound13)showsasignificantanti-inflammatoryeffectintheratantigeninducedarthritismodelafteroraladministrationat30mg/kgbidfor20days[1].NE52-QQ57(30mg/kgbidpofor4days)alsopreventsangiogenesisinthemousechambermodelaswellaspainasdemonstratedintheratcompleteFreund’sadjuvantmodel[1].AnimalModel:FemaleFVBmice(8-10weeks)[1]Dosage:30mg/kgAdministration:Oral,4days,bidResult:Treatmentat30mg/kgp.o.bidstartingonday0,thedayofthechamberimplantation,showedastatisticallysignificantreduction(46.8±10.6%)oftissuegrowthbyday4.Thebloodlevelsof13onday4at2and16haftercompoundapplicationinthismodelwere9.03±2.87and0.09±0.06μM[1].AnimalModel:MaleWistarHanrats[1]Dosage:3,10,and30mg/kgAdministration:Oral,20days,bidResult:DisplayednotonlyhigherexposuresintheratAIAbutalsolowerplasmaproteinbindinginrat(95%)[1].户使⽤本产品发表的科研⽂献•CellDeathDis.2022Feb14;13(2):152.•Preprints.2021,2021040223.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].VelcickyJ,etal.DevelopmentofSelective,OrallyActiveGPR4AntagonistswithModulatoryEffectsonNociception,Inflammation,andAngiogenesis.JMedChem.2017May11;60(9):3672-3683.[2].HosfordPS,etal.CNSdistribution,signallingpropertiesandcentraleffectsofG-proteincoupledreceptor4.Neuropharmacology.2018Aug;138:381-392.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme