Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAmentoflavoneCat.No.:HY-N0662CASNo.:1617-53-4Synonyms:Didemethyl-ginkgetin分?式:C??H??O??分?量:538.46作?靶點(diǎn):ReactiveOxygenSpecies;Apoptosis;Bacterial;Fungal;RSV;GABAReceptor作?通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis;Anti-infection;MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(232.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8571mL9.2857mL18.5715mL5mM0.3714mL1.8571mL3.7143mL10mM0.1857mL0.9286mL1.8571mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)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?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)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%salineSolubility:≥2.5mg/mL(4.64mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.64mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Amentoflavone(Didemethyl-ginkgetin)?種有效且具有?服活性的GABA(A)負(fù)調(diào)節(jié)劑。Amentoflavone還顯?出抗炎、抗氧化、抗病毒、抗腫瘤、抗輻射、抗活性。Amentoflavone誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期停滯在亞G1期[1][2][3][4]。體外研究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-?BactivationanddecreasestheexpressionofMCL1andC-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?邊的抑制劑?師www.MedChemEWesternBlotAnalysis[3]CellLine:U-87MGcellsConcentration:0,50,100μMIncubationTime:48hResult:SignificantlyreducedNF-?Bactivationinadose-dependentmannerby25-87%andreducedproteinexpressionofMCL1andC-FLIPby50-80%and38-57%,respectively.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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-?B-modulatedAnti-apoptoticSignalinginGlioblastomaCells.InVivo.2018Mar-Apr;32(2):279-285.[5].HwangJH,etal.Antibacterialeffectofamentoflavoneanditssynergisticeffectwithantibiotics.JMicrobiolBiotechnol.2013;23(7):953-8.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[6].HanrahanJR,etal.Semisyntheticpreparationofamentoflavone:AnegativemodulatoratGABA(A)receptors.BioorgMedChe