ACY-1083-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEACY-1083Cat.No.:HY-111791CASNo.:1708113-43-2分⼦式:C₁₇H₁₈F₂N₄O₂分⼦量:348.35作⽤靶点:HDAC作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:200mg/mL(574.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8707mL14.3534mL28.7068mL5mM0.5741mL2.8707mL5.7414mL10mM0.2871mL1.4353mL2.8707mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(14.35mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5mg/mL(14.35mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(14.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ACY-1083⼀种可渗透脑的选择性HDAC6抑制剂，IC50为3nM，ACY-1083对HDAC6的选择性⽐其他类别的HDAC亚型⾼260倍。ACY-1083可有效逆转化疗引起的周神经病变[1]。IC50&TargetHDAC63nM(IC50)体外研究TreatmentwithACY-1083(30and300nM)significantlyimprovescellviabilityinadose-dependentmanner[2].CellViabilityAssay[2]CellLine:Mousehippocampal(HT22)cellsConcentration:30and300nMIncubationTime:Result:Significantimprovementincellviability.体内研究ACY-1083(i.p.;10mg/kg;for7days)effectivelyrelievesCisplatin-inducedmechanicalallodyniainC57BL/6JmiceACY-1083(oraldosesof3mg/kgACY-1083for7days)reversesPaclitaxel-inducedmechanicalallodyniainadultmaleSDrats.Micedosedwith5mg/kgACY-1083byintraperitoneal(i.p.)injectionhaveamaximumplasmaconcentration(Cmax)of936ng/mL,ahalf-life(T1/2)of3.5hours,andabiologicallyactiveplasmaexposureof8hoursafterdosing.AnimalModel:AdultmaleC57BL/6Jmiceof8-10weeksofage[1]Dosage:3or10mg/kgAdministration:Administeredi.p.injection;daily;for7daysResult:The10mg/kgrelievedCisplatin(2.3mg/kg)-inducedmechanicalallodynia,whereasthe3mg/kgdosedidnot.AnimalModel:AdultmaleSpragueDawleyrats[1]Dosage:3mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Twodailydosesweregivenorallyfor7days.Result:ReversedPaclitaxel(6mg/kgor12mg/kg)-inducedmechanicalallodynia.户使⽤本产品发表的科研⽂献•Patent.US20220281814A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KrukowskiK,etal.HDAC6inhibitioneffectivelyreverseschemotherapy-inducedperipheralneuropathy.Pain.2017Jun;158(6):1126-1137.[2].VahagnCNikolian,etal.Isoform6-selectivehistonedeacetylaseinhibitionreduceslesionsizeandbrainswellingfollowingtraumaticbraininjuryandhemorrhagicshock.JTraumaAcuteCareSurg.2019Feb;86(2):232-239.McePdfHeightCaution:Producthasnotbeenfullyvalida