Eliglustat-Genz-99067-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEliglustatCat.No.:HY-14885CASNo.:491833-29-5Synonyms:Genz99067分?式:C??H??N?O?分?量:404.54作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(247.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4719mL12.3597mL24.7194mL5mM0.4944mL2.4719mL4.9439mL10mM0.2472mL1.2360mL2.4719mL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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(6.18mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.18mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.18mM);ClearsolutionBIOLOGICALACTIVITY?物活性Eliglustat?效特異，有?服活性的葡糖腦苷脂合成酶抑制劑，IC50值為24nM。IC50&TargetIC50:24nM(glucocerebrosidesynthase)[1]體外研究EliglustattartrateshowsgoodpotencywithanIC50of24nMandspecificityagainstthetargetenzyme[1].IncubatingK562orB16/F10cellsfor72hwithincreasingamountsofGenz-112638(0.6-1000nM)resultsinadose-dependentreductionofcellsurfacelevelsofbothGM1andGM3.ThemeanIC50valueforinhibitingthecellsurfacepresentationofGM1inK562cellswas24nM(range14-34nM)andthatforGM3inB16/F10cellswas29nM(range12-48nM)[1].體內(nèi)研究Micethatreceiveddrugpriortosignificantaccumulationofsubstrate(10weeksofage)showedreducedlevelsofglucosylceramideandnumberofGauchercellsinthespleen,lungandliverwhencomparedtoage-matchedcontrolanimals[1].PROTOCOLCellAssay[1]TheinhibitoryactivityofGenz-112638isdeterminedindirectlybymeasuringitseffectonthecellsurfacelevelsofthegangliosidesGM1andGM3oneitherK562orB16/F10cells.GM1levelsontheK562cellsaredeterminedbyincubatingthecellswithincreasingamountsofGenz-112638(0.6-1000nM)for72hafterwhichthecellsareharvestedandstainedusing10μgofrecombinantcholeratoxin-FITCin100μLphosphatebufferedsaline(PBS)containing0.5%bovineserumalbumin(BSA)for30minonice.Cellsareished,resuspendedinPBScontaining0.5%BSAandthefluorescencequantitated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Eliglustathemitartrateisdissolvedinwaterforinjectionandadministeredinadoseescalationfrom75Administration[1]mg/kg/dayto150mg/kg/dayoverthecourseofninedays,withthreedaysateachdoseandincrementsof25mg/kg/day.Miceareweighedthreetimesperweektomonitorthepotentialimpactofthedrugontheiroverallhealth.Animalsarekilledbycarbondioxideinhalation[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Immunity.2021Jan12;54(1):132-150.e9.?CancerDiscov.2022Nov4;CD-22-0535.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?NatCommun.2020Aug27;11(1):4279.?CellDeathDis.2021Oct6;12(10):911.?StemCellsTranslMed.2021Mar3.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].McEachernKA,etal.AspecificandpotentinhibitorofglucosylceramidesynthaseforsubstrateinhibitiontherapyofGaucherdisease.MolGenetMetab.2007Jul;91(3):259-68.McePdfHeightCaution:Pr