Emixustat-ACU-4429-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEmixustatCat.No.:HY-19720CASNo.:1141777-14-1Synonyms:ACU-4429分?式:C??H??NO?分?量:263.38作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)Ethanol:100mg/mL(379.68mM;Needultrasonic)DMSO:≥43mg/mL(163.26mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.7968mL18.9840mL37.9680mL5mM0.7594mL3.7968mL7.5936mL10mM0.3797mL1.8984mL3.7968mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%EtOH>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3mg/mL(11.39mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥3mg/mL(11.39mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%EtOH>>90%cornoilSolubility:≥3mg/mL(11.39mM);ClearsolutionBIOLOGICALACTIVITY?物活性Emixustat新穎的視覺周期調(diào)節(jié)器，視覺周期異構(gòu)酶的抑制劑，體外實(shí)驗(yàn)的IC50值為4.4nM。IC50&TargetIC50:4.4nM(visualcycleisomerase)[1]體外研究Emixustatpotentlyinhibitsisomeraseactivityinvitro(IC50=4.4nM).Treatmentofemixustatshowsaconcentrationdependentreductionof11-cis-ROLproduction[1].Emixustatstronglyinhibits11-cis-retinolproductionwithanIC50valueof232±3nM[2].體內(nèi)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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfully