Amentoflavone-Didemethyl-ginkgetin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAmentoflavoneCat.No.:HY-N0662CASNo.:1617-53-4Synonyms:Didemethyl-ginkgetin分⼦式:C₃₀H₁₈O₁₀分⼦量:538.46作⽤靶点:ReactiveOxygenSpecies;Apoptosis;Bacterial;Fungal;RSV;GABAReceptor作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis;Anti-infection;MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(232.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8571mL9.2857mL18.5715mL5mM0.3714mL1.8571mL3.7143mL10mM0.1857mL0.9286mL1.8571mL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1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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:≥2.5mg/mL(4.64mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.64mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Amentoflavone(Didemethyl-ginkgetin)⼀种有效且具有⼝服活性的GABA(A)负调节剂。Amentoflavone还显⽰出抗炎、抗氧化、抗病毒、抗肿瘤、抗辐射、抗活性。Amentoflavone诱导细胞凋亡(apoptosis)和细胞周期停滞在亚G1期[1][2][3][4]。体外研究Amentoflavone(1-60µM)inhibitstheproductionofnitricoxideinaconcentration-dependentmannerinRAW264.7cells[2].Amentoflavone(50-200µM)inhibitstheviabilityofU-87MGcellswithIC50valueof100µMat48h[3].Amentoflavone(0,50,100µM;48h)inducesapoptosisandcellcyclearrestatsub-G1phase[3].Amentoflavone(0,50,100µM;48h)inhibitsNF-ĸBactivationanddecreasestheexpressionofMCL1andC-FLIPproteininU-87MGcells[3].Amentoflavone(0-32µg/ml)showsantibacterialactivitywithMICsof8,4,32,8,16,8µg/mlforE.faeciumATCC19434,S.aureusATCC25923,S.mutansATCC3065,E.coliO-157ATCC25922,E.coliATCC43895,P.aeruginosaATCC27853,respectively[4].CellViabilityAssay[3]CellLine:U-87MGcellsConcentration:0,50,75,100,200µMIncubationTime:48hResult:SignificantlyinhibitedtheviabilityofU-87MGcellsby23-71%withanIC50valueof100µMat48h.ApoptosisAnalysis[3]CellLine:U-87MGcellsConcentration:0,50,100µMIncubationTime:48hResult:Significantlyinducedtheaccumulationofcellsinthesub-G1populationandincreasedthelevelofactivecaspase-3by14-52%and24-42%,respectively,andsignificantlytriggeredthelossofΨmandtheexpressionofactivecaspase-8by23-53%and25-50%,respectively.2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEWesternBlotAnalysis[3]CellLine:U-87MGcellsConcentration:0,50,100µMIncubationTime:48hResult:SignificantlyreducedNF-ĸBactivationinadose-dependentmannerby25-87%andreducedproteinexpressionofMCL1andC-FLIPby50-80%and38-57%,respectively.体内研究Amentoflavone(25mg/kg;p.o.;onceadayfor3consecutivedays)showsneuroprotectiveroleinepilepsyviaanti-inflammatoryeffectsinmouse[1].AnimalModel:5-6weeks,28-32g,kunmingmice[1]Dosage:25mg/kgAdministration:P.o.;onceadayfor3consecutivedaysResult:InhibitedactivationandnucleartranslocationofNF-κBsubunitsp65,decreasedIL-6andIL-1βproductionandsignificantlydecreasedNOandprostaglandinE2production.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•PharmacolRes.2020May;155:104751.•JMedChem.2021Aug18.•LifeSci.2020Apr15;247:117425.•AnticancerRes.2021,41(3)1357-1364.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangZ,etal.Amentoflavoneprotectshippocampalneurons:anti-inflammatory,antioxidative,andantiapoptoticeffects.NeuralRegenRes.2015Jul;10(7):1125-33.[2].WooER,etal.AmentoflavoneinhibitstheinductionofnitricoxidesynthasebyinhibitingNF-kappaBactivationinmacrophages.PharmacolRes.2005Jun;51(6):539-46.[3].WooER,etal.AmentoflavoneinhibitstheinductionofnitricoxidesynthasebyinhibitingNF-kappaBactivationinmacrophages.PharmacolRes.2005Jun;51(6):539-46.[4].YenTH,etal.AmentoflavoneInducesApoptosisandInhibitsNF-ĸB-modulatedAnti-apoptoticSignalinginGlioblastomaCells.InVivo.2018Mar-Apr;32(2):279-285.[5].HwangJH,etal.Antibacterialeffectofamentoflavoneanditssynergisticeffectwithantibiotics.JMicrobiolBiotechnol.2013;23(7):953-8.3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[6].HanrahanJR,etal.Semisyntheticpreparationofamentoflavone:AnegativemodulatoratGABA(A)receptors.BioorgMedChe