Puerarin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPuerarinCat.No.:HY-N0145CASNo.:3681-99-0分?式:C??H??O?分?量:416.38作?靶點(diǎn):5-HTReceptor作?通路:GPCR/GProtein;NeuronalSignaling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:50mg/mL(120.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4017mL12.0083mL24.0165mL5mM0.4803mL2.4017mL4.8033mL10mM0.2402mL1.2008mL2.4017mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3mg/mL(7.20mM);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:≥3mg/mL(7.20mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:3mg/mL(7.20mM);Suspendedsolution;Needultrasonic4.請(qǐng)依序添加每種溶劑：20%SBE-β-CDinsalineSolubility:20mg/mL(48.03mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性葛根素從葛根中提取的異酮，5-HT2C受體拮抗劑。IC50&Target5-HT2CReceptor體外研究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].體內(nèi)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?邊的抑制劑?師www.MedChemEMice:FortymaleICRmice(weight:20-22g)areacclimatizedwithadaily12hlight:12hdarkcycleat22±2°Croomtemperatureand55%±5%relativehumidity.After1weekofadaption,themicearerandomLydividedintofourgroupswithtenmicepergroup.Genisteinandpuerarinareappliedtothemiceinsodiumcarboxymethylcellulosesolutionwithanequimolarconcentrationof0.1M(gastricvolume:3mLkg-1bodyweight)[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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