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Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOxymatrineCat.No.:HY-N0158CASNo.:16837-52-8分⼦式:C₁₅H₂₄N₂O₂分⼦量:264.36作⽤靶点:TGF-beta/Smad;Apoptosis作⽤通路:StemCell/Wnt;TGF-beta/Smad;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(378.27mM;Needultrasonic)H2O:100mg/mL(378.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7827mL18.9136mL37.8272mL5mM0.7565mL3.7827mL7.5654mL10mM0.3783mL1.8914mL3.7827mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(9.46mM);Clearsolution2.请依序添加每种溶剂:10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.46mM);Clearsolution3.请依序添加每种溶剂:10%DMSO>>90%cornoilSolubility:2.5mg/mL(9.46mM);Clearsolution;Needwarming4.请依序添加每种溶剂:PBSSolubility:100mg/mL(378.27mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Oxymatrine来⾃苦参的⽣物碱,具有抗炎,抗纤维化和抗肿瘤的作⽤。Oxymatrine能抑制iNOS表达和TGF-β/Smad通路。Oxymatrine可抑制博卡病毒MVC复制,降低病毒因表达并减少病毒感染诱导的细胞凋亡(apoptosis)。体外研究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].体内研究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—您⾝边的抑制剂⼤师www.MedChemEThetreatedratsreceiveOxymatrineceliacinjectionsat10mg/kgtwiceaweekbesidestheinjectionofCCl4[3].Mice:BALB/chomozygous(nu/nu)nudemiceareusedinthestudy.24tumor-bearingmicearerandomLydividedintothreegroups:ThecontrolgroupistreatedwithPBS,andtwogroupsaretreatedwithdifferentconcentrationsofoxymatrine(50mg/kgand100mg/kgbodyweight).Oxymatrineisadministeredtothemice,usingdailyintraperitonealinjections[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•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

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