Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEACY-1083Cat.No.:HY-111791CASNo.:1708113-43-2分?式:C??H??F?N?O?分?量:348.35作?靶點:HDAC作?通路:CellCycle/DNADamage;Epigenetics儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(574.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8707mL14.3534mL28.7068mL5mM0.5741mL2.8707mL5.7414mL10mM0.2871mL1.4353mL2.8707mL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(storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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、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:≥5mg/mL(14.35mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5mg/mL(14.35mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(14.35mM);ClearsolutionBIOLOGICALACTIVITY?物活性ACY-1083?種可滲透腦的選擇性HDAC6抑制劑，IC50為3nM，ACY-1083對HDAC6的選擇性?其他類別的HDAC亞型?260倍。ACY-1083可有效逆轉(zhuǎn)化療引起的周神經(jīng)病變[1]。IC50&TargetHDAC63nM(IC50)體外研究TreatmentwithACY-1083(30and300nM)significantlyimprovescellviabilityinadose-dependentmanner[2].CellViabilityAssay[2]CellLine:Mousehippocampal(HT22)cellsConcentration:30and300nMIncubationTime:Result:Significantimprovementincellviability.體內(nèi)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?邊的抑制劑?師www.MedChemEAdministration:Twodailydosesweregivenorallyfor7days.Result:ReversedPaclitaxel(6mg/kgor12mg/kg)-inducedmechanicalallodynia.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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