Palmatine-hydroxide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPalmatinehydroxideCat.No.:HY-N0110BCASNo.:131-04-4分⼦式:C₂₁H₂₃NO₅分⼦量:369.41作⽤靶点:Indoleamine2,3-Dioxygenase(IDO);VirusProtease;AuroraKinase;Apoptosis;Bacterial;Parasite作⽤通路:MetabolicEnzyme/Protease;Anti-infection;CellCycle/DNADamage;Epigenetics;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:15.62mg/mL(42.28mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7070mL13.5351mL27.0702mL5mM0.5414mL2.7070mL5.4140mL10mM0.2707mL1.3535mL2.7070mL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。BIOLOGICALACTIVITY⽣物活性Palmatinehydroxide⼀种具有⼝服活性的、不可逆的IDO-1抑制剂，对HEK293-hIDO-1和rhIDO-1的IC50分别为3μM和157μM。Palmatinehydroxide也能⾮竞争性抑制西尼罗病毒(WNV)NS2B-NS3蛋⽩酶，IC50为96μM。Palmatinehydroxide具有抗癌、抗炎、神经保护、抗细、抗病毒活性。1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetIDO-1IDO-1WNVNS2B-NS33μM(IC50,HEK293-hIDO-1)157μM(IC50,rhIDO-1)96μM(IC50)体外研究Palmatine(0-100μM;42h)suppressesWNVwithanEC50valueof3.6μM,andreducetheviraltitersofDENV-2andYFVwithEC50valuesof26.4μMand7.3μM,respectively[3].Palmatine(0-1128μM;24-72h)inhibitscoloncancercellproliferation[5].Palmatine(0-704μM;24h)reducesAURKAproteinlevels,inducesG2/Mphasearrest,andinducesapoptosisincoloncancercellsviathemitochondrialassociatedpathway[5].CellProliferationAssay[5]CellLine:HCT-116,SW480,HT-29Concentration:0,88,176,352,and704μM(HCT-116,SW480);0,141,282,564,and1128μM(HT-29)IncubationTime:24,48and72hResult:Decreasedcellviabilityinadose-dependentmanner.WesternBlotAnalysis[5]CellLine:HCT-116,SW480,HT-29Concentration:100nMforHCT-116,500nMforSW480andHT-29IncubationTime:24,48and72hResult:PromotedtheexpressionofapoptosismarkerssuchasP53/P73,Caspase3,andCaspase9.ReducedAURKAproteinlevels.Increasedcyt.cinthecytoplasmwhilereducedBcl2andBcl-xlinadose-dependentmanner.CellCycleAnalysis[5]CellLine:HCT-116,SW480Concentration:88,176,352and704μMIncubationTime:24,48and72hResult:InducedG2/Mphasearrestinadose-dependentmanner.ApoptosisAnalysis[5]CellLine:HCT-116,SW480Concentration:88,176,352and704μMIncubationTime:24,48and72hResult:Inducedapoptosisinadose-dependentmanner.2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究Palmatine(50or100mg/kg;p.o.;dailyfor7days)amelioratesDSS(dextransulfatesodium)-inducedcolitisandpreventsinfiltrationofinflammatorycells[1].Palmatine(0-200mg/kg;i.p.;once)attenuatesD-galactosamine/Lipopolysaccharides(HY-D1056)-inducedfulminanthepaticfailureinmice[2].Palmatine(0-1mg/kg;i.p.;10days)showsmemory-enhancingactivityinmice[4].Palmatine(33.75-135mg/kg;p.o.;dailyfor26days)caneffectivelyinhibitthegrowthofHCT-116xenograftsinmice[5].AnimalModel:DSS-inducedColitisBALB/cmicemodel(8-week-old)[1]Dosage:50or100mg/kgAdministration:Orally,daily,for7daysResult:AmelioratedDSS-inducedcolitisandpreventedinfiltrationofinflammatorycells;remarkablyextendedthecolonlength;significantlysuppressedthecolonicMPOactivity.Decreasedthelevelsofcolonicinflammatorycytokines(TNF-α,IFN-γ,IL-1β,IL-6,IL-4andIL-10);ProtectedmucosalintegritybymodulatingTJsproteinandapoptosisproteins;RestoredDSS-induceddecreasesofTJproteinZO-1,ZO-2andclaudin-1;ReducedBaxexpressionandenhancedBcl-2expressionatthedoseof100ꢀmg/kg,preventedepithelialapoptosisandimprovedintestinalintegrity.PreventedDSS-inducedchangesofgutmicrobiotaincolitismice.AnimalModel:MaleICRmice(20–22g),D-galactosamine/lipopolysaccharide(GalN/LPS)-inducedfulminanthepaticfailuremodel[2]Dosage:25,50,100,or200mg/kgAdministration:Intraperitonealinjection,1hbeforetheGalN/LPStreatmentResult:AttenuatedthemortalityandserumaminotransferaseactivitiesincreasedbyGalN/LPS.PreventedtheincreaseofserumTNF-αandaugmentedthatofserumIL-10.DecreasedtheTNF-amRNAexpressionandincreasedtheIL-10mRNAexpression.Attenuatedtheapoptosisofhepatocytes.AnimalModel:Swissyoungmalealbinomice,withScopolamine(HY-N0296)-anddiazepam-inducedamnesiamodel[4]Dosage:0.1,0.5,1mg/kgAdministration:Intraperitonealinjection,10daysResult:Significantlyimprovedlearningandmemoryofmiceat0.5and1mg/kganddidnotshowanysignificanteffectonlocomotoractivityofthemice.Significantlyreversedscopolamine-anddiazepam-inducedamnesiainmice.Significantlyreducedbrainacetylcholinesteraseactivityofmice.3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:BALB/c-nudemice,HCT-116xenograftmodel[5]Dosage:33.75,67.5and135mg/kgAdministration:Oraladministration,onceadayfor26daysResult:Thetumorvolumeandweightofthetreatmentgroupweresignificantlyreduced.户使⽤本产品发表的科研⽂献•OxidMedCellLongev.2021Mar13.•IntImmunopharmacol.2022Feb9;106:108583.•BiolRes.2020Sep14;53(1):39.•DrugDevRes.2022Aug17.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangXJ,etal.Palmatineamelioratedmurinecolitisbysuppressingtryptophanmetabolismandregulatinggutmicrobiota.PharmacolRes.2018Nov;137:34-46.[2].LeeWC,etal.PalmatineattenuatesD-galactosamine/lipopolysaccharide-inducedfulminanthepaticfailureinmice.FoodChemToxicol.2010Jan;48(1):222-8.[3].JiaF,etal.IdentificationofpalmatineasaninhibitorofWestNilevirus.ArchVirol.2010Aug;155(8):1325-9.[4].DhingraD,etal.Memor