Atraric-acid-Methyl-atrarate-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAtraricacidCat.No.:HY-N2908CASNo.:4707-47-5Synonyms:Methylatrarate分⼦式:C₁₀H₁₂O₄分⼦量:196.2作⽤靶点:AndrogenReceptor;NOSynthase;p38MAPK;NF-κB作⽤通路:VitaminDRelated/NuclearReceptor;Immunology/Inflammation;MAPK/ERKPathway;NF-κB储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(509.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.0968mL25.4842mL50.9684mL5mM1.0194mL5.0968mL10.1937mL10mM0.5097mL2.5484mL5.0968mL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(storedundernitrogen)。-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>>90%cornoil1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(12.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Atraricacid(Methylatrarate)⼀种特异的雄激素受体(androgenreceptor)拮抗剂，具有抗炎和抗癌作⽤。Atraricacid抑制LNCaP和C4-2细胞中内性前列腺特异性抗原因的表达。Atraricacid还能抑制NO和细胞因⼦的合成，抑制MAPK-NFκB信号通路。Atraricacid可⽤于前列腺疾病和炎症性疾病的研究。IC50&TargetAndrogenreceptor,NOsynthesis,MAPK-NFκBpathway[1][2]体外研究Atraricacid(10μM;CV1cells)repressesthetransactivationfunctionmediatedbyDihydrotestosterone-inducedhumanAR[1].Atraricacid(10μM;PCacells)inhibitstheexpressionofthePSAgeneinbothandrogen-dependentandandrogen-independentPCacells[1].Atraricacid(1-300μM;24h)dose-dependentlyinhibitspro-inflammatorycytokine,nitricoxide,prostaglandinE2inLPS-stimulatedRAW264.7cells,butdoesnotinfluencethecellviability[2].Atraricacid(100and300μM;18hor4h)downregulatestheexpressionofphosphorylatedIκB,extracellularsignal-regulatedkinases(ERK)andnuclearfactorkappaB(NFκB)signalingpathwaytoexhibitanti-inflammatoryeffectsinLPS-stimulatedRAW264.7cells[2].CellViabilityAssay[2]CellLine:RAW264.7cellsConcentration:1-300μMIncubationTime:24hResult:Didnotinfluencethecellviability.WesternBlotAnalysis[2]CellLine:RAW264.7cellsConcentration:100and300μMIncubationTime:18hor4hResult:InhibitedLPS-InducedexpressionofiNOSandCOX-2inadose-dependentmanner.SuppressedLPS-stimulatedphosphorylationoftheNfκbsignalingpathway.体内研究Atraricacid(10,30mg/kg;i.p.;singledosage)inhibitstheproductionofpro-inflammatorycytokinesandreducespathologicaldamagesinLPS-inducedendotoxinshockmice[2].AnimalModel:FemaleBALB/cmice(7weeksold,17-20g;LPS-inducedendotoxinshock)[2]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDosage:10,30mg/kgAdministration:i.p.;singledosageResult:Inhibitedtheproductionofpro-inflammatorycytokines.Reducedpathologicaldamagessuchasvasodilationandbleeding.REFERENCES[1].RoellD,BaniahmadA.ThenaturalcompoundsatraricacidandN-butylbenzene-sulfonamideasantagonistsofthehumanandrogenreceptorandinhibitorsofprostatecancercellgrowth.MolCellEndocrinol.2011Jan30;332(1-2):1-8.[2].PapaioannouM,etal.Thenaturalcompoundatraricacidisanantagonistofthehumanandrogenreceptorinhibitingcellularinvasivenessandprostatecancercellgrowth.JCellMolMed.2009Aug;13(8B):2210-2223.McePdfHeightCaution:Producthasno