Emixustat-ACU-4429-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEmixustatCat.No.:HY-19720CASNo.:1141777-14-1Synonyms:ACU-4429分⼦式:C₁₆H₂₅NO₂分⼦量:263.38作⽤靶点:Others作⽤通路:Others储存⽅式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Ethanol:100mg/mL(379.68mM;Needultrasonic)DMSO:≥43mg/mL(163.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7968mL18.9840mL37.9680mL5mM0.7594mL3.7968mL7.5936mL10mM0.3797mL1.8984mL3.7968mL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。-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1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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%EtOH>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3mg/mL(11.39mM);Clearsolution2.请依序添加每种溶剂：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥3mg/mL(11.39mM);Clearsolution3.请依序添加每种溶剂：10%EtOH>>90%cornoilSolubility:≥3mg/mL(11.39mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Emixustat新颖的视觉周期调节器，视觉周期异构酶的抑制剂，体外实验的IC50值为4.4nM。IC50&TargetIC50:4.4nM(visualcycleisomerase)[1]体外研究Emixustatpotentlyinhibitsisomeraseactivityinvitro(IC50=4.4nM).Treatmentofemixustatshowsaconcentrationdependentreductionof11-cis-ROLproduction[1].Emixustatstronglyinhibits11-cis-retinolproductionwithanIC50valueof232±3nM[2].体内研究Emixustatreducestheproductionofvisualchromophore(11-cisretinal)inwild-typemicefollowingasingleoraldose(ED50=0.18mg/kg).Inalbinomice,emixustatisshowntobeeffectiveinpreventingphotoreceptorcelldeathcausedbyintenselightexposure.Pre-treatmentwithasingledoseofemixustat(0.3mg/kg)providsa50%protectiveeffectagainstlight-inducedphotoreceptorcellloss,whilehigherdoses(1-3mg/kg)arenearly100%effective.InAbca4-/-mice,chronic(3month)emixustattreatmentmarkedlyreduceslipofuscinautofluorescenceandreducesA2Elevelsby60%(ED50=0.47mg/kg).Intheretinopathyofprematurityrodentmodel,treatmentwithemixustatduringtheperiodofischemiaandreperfusioninjuryproducesa30%reductioninretinalneovascularization(ED50=0.46mg/kg)[1].PROTOCOLAnimalMice:Albino(BALB/c)miceareusedtoassesstheeffectsofemixustatonprotectionfromlightdamage.Administration[1]Micearetreatedwithasingledoseofemixustat(0.3mg/kgand1.0mg/kg).TheeffectofemixustatontheaccumulationofA2EandlipofuscinautofluorescenceisexaminedinAbca4-/-mice.Micearetreatedwithemixustat(3monthsdailytreatment,0.3or3mg/kg/day)[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].BavikC,etal.VisualCycleModulationasanApproachtowardPreservationofRetinalIntegrity.PLoSOne.2015May13;10(5):e0124940.[2].KiserPD,etal.Catalyticmechanismofaretinoidisomeraseessentialforvertebratevision.NatChemBiol.2015Jun;11(6):409-15.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfully