Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOxymatrineCat.No.:HY-N0158CASNo.:16837-52-8分?式:C??H??N?O?分?量:264.36作?靶點:TGF-beta/Smad;Apoptosis作?通路:StemCell/Wnt;TGF-beta/Smad;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:100mg/mL(378.27mM;Needultrasonic)H2O:100mg/mL(378.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.7827mL18.9136mL37.8272mL5mM0.7565mL3.7827mL7.5654mL10mM0.3783mL1.8914mL3.7827mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(9.46mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.46mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:2.5mg/mL(9.46mM);Clearsolution;Needwarming4.請依序添加每種溶劑：PBSSolubility:100mg/mL(378.27mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Oxymatrine來?苦參的?物堿，具有抗炎，抗纖維化和抗腫瘤的作?。Oxymatrine能抑制iNOS表達和TGF-β/Smad通路。Oxymatrine可抑制博卡病毒MVC復制，降低病毒因表達并減少病毒感染誘導的細胞凋亡(apoptosis)。體外研究Oxymatrine,analkaloidcomponentextractedfromtherootsofSophoraspecies,hasbeenshowntohaveantiinflammatory,antifibrosis,andantitumoreffectsandtheabilitytoprotectagainstmyocardialdamage,etc.ThepotentialsignalingpathwaysinvolvedintheclinicalapplicationofoxymatrinemightincludetheTGF-β/Smad,tolllikereceptor4/nuclearfactorkappa-light-chain-enhancerofactivatedBcells,toll-likereceptor9/TRAF6,Januskinase/signaltransductionandactivatoroftranscription,phosphatidylinositol-3kinase/Akt,delta-opioidreceptorarrestinl-Bcl-2,CD40,epidermalgrowthfactorreceptor,nuclearfactorerythroid-2-relatedfactor2/hemeoxygenase-1signalingpathways,anddimethylargininedimethylaminohydrolase/asymmetricdimethylargininemetabolismpathway[1].OxymatrinesignificantlyinhibitstheproliferationofDU145andPC-3celllinesinatime-anddose-dependentmanner.Bycontrast,followingtreatmentwithoxymatrine,PNT1Bhealthyhumanprostatecellproliferationisnotinhibited[2].體內研究Thevolumeandweightoftumorsinmicesignificantlydecreasedinadose-dependentmanner.Oxymatrinemayreduceprostatecancercellgrowthbypromotingcellapoptosisinvivo[2].Oxymatrineiseffectiveinreducingtheproductionanddepositionofcollageninthelivertissueofexperimentalrats.OxymatrinecouldpromotetheexpressionofSmad7andinhibittheexpressionofSmad3andCBPinCCl4-inducedhepaticfibrosisinSDrats,couldmodulatethefibrogenicsignaltransductionofTGFβ-Smadpathway[3].PROTOCOLCellAssay[2]DU145,PC-3andPNT1Bcelllines(3×104cells/well)areseededinto96-wellplatesandincubatedovernightat37°Cin5%CO2.Subsequently,thecellsareincubatedwithdifferentconcentrationsofoxymatrine(0,2,4,6and8mg/mL).MTT(10mL;5mg/mL)isaddedandthemixtureisincubatedindarknessat37°Cfor2h.Absorbanceismeasuredatawavelengthof490nmusingamicroplatereader[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:OnehundredhealthymaleSDrats(weight140-160g)areusedinthestudy.All100ratsarerandomLyAdministration[2][3]dividedintothreegroups:Control(n=20),Treatment(n=40)andModelgroup(n=40).Forthemodelgroup,300g/LCCl4solutedinliquidparaffinisinjectedsubcutaneouslyatadosageof3mL/kgtwiceperweek[6].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEThetreatedratsreceiveOxymatrineceliacinjectionsat10mg/kgtwiceaweekbesidestheinjectionofCCl4[3].Mice:BALB/chomozygous(nu/nu)nudemiceareusedinthestudy.24tumor-bearingmicearerandomLydividedintothreegroups:ThecontrolgroupistreatedwithPBS,andtwogroupsaretreatedwithdifferentconcentrationsofoxymatrine(50mg/kgand100mg/kgbodyweight).Oxymatrineisadministeredtothemice,usingdailyintraperitonealinjections[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發(fā)表的科研?獻?CellDeathDis.2020Aug10;11(8):695.?JMedChem.2019Sep12;62(17):7961-7975.?LifeSci.2020Sep15;257:118090.?FrontBioengBiotechnol.2020May8;8:392.?IntImmunopharmacol.2021Sep10;100:108139.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LuML,etal.PotentialSignalingPathwaysInvolvedintheClinicalApplicationofOxymatrine.PhytotherRes.2016Jul;30(7):1104-12.[2].WuC,etal.Oxymatrineinhibitstheproliferationofprostatecancercellsinvitroandinvivo.MolMedRep.2015Jun;11(6):4129-34.[3].WuXL,etal.EffectofOxymatrineontheTGFbeta-SmadsignalingpathwayinratswithCCl4-inducedhepaticfibrosis.WorldJGastroenterol.2008Apr7;14(13):2100-5.[4].DingY,etal.OxymatrineInhibitsBocavirusMVCReplication,ReducesViralGeneExpressionandDecreasesApoptosi