Puerarin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPuerarinCat.No.:HY-N0145CASNo.:3681-99-0分⼦式:C₂₁H₂₀O₉分⼦量:416.38作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(120.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4017mL12.0083mL24.0165mL5mM0.4803mL2.4017mL4.8033mL10mM0.2402mL1.2008mL2.4017mL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:≥3mg/mL(7.20mM);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:≥3mg/mL(7.20mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:3mg/mL(7.20mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：20%SBE-β-CDinsalineSolubility:20mg/mL(48.03mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性葛根素从葛根中提取的异酮，5-HT2C受体拮抗剂。IC50&Target5-HT2CReceptor体外研究PuerarininhibitstheexpressionofLPS-inducediNOS,COX-2andCRPproteinsandalsosuppressestheirmRNAsfromRT-PCRexperimentsinRAW264.7cells.TheinhibitionofiNOS,COX-2andCRPexpressionisduetoadose-dependentinhibitionofphosphorylationanddegradationofI-κB,whichresultedinthereductionofp65NF-κBnucleartranslocation.Theeffectofpuerarin-mediatedinhibitionofLPS-inducediNOS,COX-2andCRPexpressionisattributedtosuppressedNF-κBactivationatthetranscriptionallevel[1].Puerarinisanovelopen-channelblockerofIK1,whichmayunderlietheantiarrhythmicactionofpuerarin.Puerarincompeteswithbarium,anopen-channelblockerofIK1,toinhibitIK1currents[2].体内研究Bothgenisteinandpuerarineffectivelyalleviatehepaticdamageinducedbychronicalcoholadministrationthroughpotentialantioxidant,anti-inflammatory,orantiapoptoticmechanisms.However,genisteinismoreeffectivethanpuerarinindecreasinglevelsofmalondialdehyde(1.05±0.0947vs.1.28±0.213nmol/mgpro,p[3].Early-stagerenaldamagescanbesignificantlyimprovedbypuerarin,possiblyviaitssuppressionofICAM-1andTNF-αexpressionindiabeticratkidneys[4].PROTOCOLCellAssay[1]RAW264.7cellsaremaintainedatsubconfluencein95%airand5%CO2humidifiedatmospheremaintainedat37°C.ThemediumusedforroutinesubcultureisDulbecco’sModifiedEagle’sMediumsupplementedwith10%fetalbovineserum,penicillin(100units/mL)andstreptomycin(100μg/mL).AnMTTassayisusedtomeasuretheviabilityofthecellsaftertreatmentwithpuerarin.Afterthesupernatantsareremovedfornitritedetermination,cellsareincubatedat37°CwithMTT(0.05mg/mL)for4h,andtheopticaldensityismeasuredat540nm.Theconcentrationsofpuerarinare10,20,40and100μM[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:AcohortofhealthymaleSDrats(7weeksold)arerandomLydividedintoacontrolgroup,amodelAdministration[3][4]group,andapuerarintreatmentgroupwithhigh(H),moderate(M),andlow(L)dosage.Puerarinisre-suspendedin0.9%salineandisgivenbyintra-gastricintubationatvariousconcentrations(0.25mg/(kg×d)forLgroup,0.5mg/(kg×d)forMgroup,and1.0mg/(kg×d)forHgroup)eachdayfor8consecutivedays.Anequalvolumeofsalineisadministeredtocontrolandmodelratsduringthesametimeperiod[4].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMice:FortymaleICRmice(weight:20-22g)areacclimatizedwithadaily12hlight:12hdarkcycleat22±2°Croomtemperatureand55%±5%relativehumidity.After1weekofadaption,themicearerandomLydividedintofourgroupswithtenmicepergroup.Genisteinandpuerarinareappliedtothemiceinsodiumcarboxymethylcellulosesolutionwithanequimolarconcentrationof0.1M(gastricvolume:3mLkg-1bodyweight)[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•FreeRadicBiolMed.2022Aug5;S0891-5849(22)00508-1.•PhytotherRes.2022Jul24.•JEthnopharmacol.8November2021,114786.•MolMedRep.2019Apr;19(4):2876-2882.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HuW,etal.PuerarininhibitsiNOS,COX-2andCRPexpressionviasuppressionofNF-κBactivationinLPS-inducedRAW264.7macrophagecells.PharmacolRep.2011;63(3):781-9.[2].ZhangH,etal.Puerarin:anovelantagonisttoinwardrectifierpotassiumchannel(IK1).MolCellBiochem.2011Jun;352(1-2):117-23.[3].ZhaoL,etal.ProtectiveEffectsofGenisteinandPuerarinagainstChronicAlcohol-InducedLiverInjuryinMiceviaAntioxidant,Anti-inflammatory,andAnti-apoptoticMechanisms.JAgricFoodChem.2016Sep28;64(38):7291-7.[4].PanX,etal.EffectofPuerarinonExpressionofICAM-1andTNF-αinKidne