Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENE52-QQ57Cat.No.:HY-101784CASNo.:1401728-56-0分?式:C??H??N?O分?量:416.52作?靶點(diǎn):GPR4作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:20mg/mL(48.02mM;ultrasonicandwarmingandadjustpHto5withHClandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4008mL12.0042mL24.0085mL5mM0.4802mL2.4008mL4.8017mL10mM0.2401mL1.2004mL2.4008mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)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:≥2mg/mL(4.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(4.80mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2mg/mL(4.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性NE52-QQ57選擇性，有?服活性的GPR4拮抗劑，IC50為70nM[1]。NE52-QQ57具有抗炎活性[1]。IC50&TargetIC50:70nM(GPR4)[1].體外研究NE52-QQ57effectivelyblocksGPR4-mediatedcAMPaccumulation(IC5026.8?nMinHEK293?cells)[2].體內(nèi)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].戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellDeathDis.2022Feb14;13(2):152.?Preprints.2021,2021040223.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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