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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMethyl-β-cyclodextrinCat.No.:HY-101461CASNo.:128446-36-6Synonyms:Methyl-beta-cyclodextrin作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mLH2O:≥50mg/mL*"≥"meanssoluble,butsaturationunknown.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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑:10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(InfinitymM);Clearsolution2.請(qǐng)依序添加每種溶劑:10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(InfinitymM);Clearsolution3.請(qǐng)依序添加每種溶劑:10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(InfinitymM);Clearsolution4.請(qǐng)依序添加每種溶劑:PBSSolubility:≥100mg/mL(InfinitymM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Methyl-β-cyclodextrin(Methyl-beta-cyclodextrin)?種環(huán)庚糖,對(duì)?極性物質(zhì)有增溶作?,?泛應(yīng)?于疏?性藥物的釋放。Methyl-β-cyclodextrin(Methyl-beta-cyclodextrin)也?泛?作降膽醇劑。Methyl-β-cyclodextrin可顯著降低?格蛋?依賴性內(nèi)吞作?。Methyl-β-cyclodextrin可阻斷細(xì)胞遷移體的形成。體外研究Methyl-β-cyclodextrinisextensivelyusedtoincreasethepermeabilityofcells,andtherebyincreasetheuptakeofsmallmoleculessuchasglucoseandnano-particles[4].Cyclodextrinsareafamilyofcyclicoligosaccharideswithahydrophilicoutersurfaceandalipophiliccentralcavity.Cyclodextrinsmoleculesarerelativelylargewithanumberofhydrogendonorsandacceptorsand,thusingeneral,theydonotpermeatelipophilicmembranes.Inthepharmaceuticalindustry,cyclodextrinshavemainlybeenusedascomplexingagentstoincreaseaqueoussolubilityofpoorlysolubledrugsandtoincreasetheirbioavailabilityandstability.Cyclodextrinsareusedinpharmaceuticalapplicationsfornumerouspurposes,includingimprovingthebioavailabilityofdrugs[4].Methyl-β-cyclodextrinquicklyinducescaspase-dependentapoptosisinPELcellsviacholesteroldepletionfromtheplasmamembrane.Methyl-β-cyclodextrininhibitsthegrowthofallPELcelllinesinadose-dependentmanner.TheIC50is3.33-4.23mMineachcellline[5].Methyl-β-cyclodextrinisahighlywatersolublecyclicheptasaccharideconsistingofaβ-glucopyranoseunit,hasbeenreportedasthemosteffectiveagentforthedepletionofcholesterolfromcellsamongthevariouscholesterol-depletingagents[5].體內(nèi)研究InaPELxenograftmousemodel,Methyl-β-cyclodextrinsignificantlyinhibitsthegrowthandinvasionofPELcellswithoutapparentadverseeffects.Methyl-β-cyclodextrin-treatedmiceappearstobehealthy,whereasnon-treatedmicehasadistendedabdominalregion.ThebodyweightsofcontrolaresignificantlyhigherthanthoseofMethyl-β-cyclodextrintreatedmice.Methyl-β-cyclodextrin-treatedmicehasasignificantlylowervolumeofascitesthanthatofnon-treatedmice[4].Studiesinbothhumansandanimalshaveshownthatcyclodextrinscanbeusedtoimprovedrugdeliveryfromalmostanytypeofdrugformulation.Currently,thereareapproximately30differentpharmaceuticalproductsworldwidecontainingdrug/cyclodextrinscomplexesinthemarket[6].PROTOCOLCellAssay[1]PELcellsareincubatedintriplicateina96-wellmicrocultureplateinthepresenceofdifferentconcentrationsofmethyl-β-cyclodextrin(0-10mM)inafinalvolumeof0.1mLfor24hat37°C.Subsequently,MTT(0.5mg/mLfinalconcentration)isaddedtoeachwell.After3hofadditionalincubation,100μLofa0.04NHClisaddedtodissolvethecrystals.Absorptionvaluesat570nmaredetermined[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:FemaleNRJmiceareintraperitoneallyinoculatedwithBCBL-1cellssuspendedinPBS.ThemiceareAdministration[1]thentreatedwithintraperitonealinjectionsofPBSormethyl-β-cyclodextrin(500mg/kgperday).Tumorburdensareevaluatedbymeasuringbodyweightsandascites[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Nature.2022Mar;603(7899):159-165.?CellRes.2021Sep;31(9):980-997.?AdvMater.2022Jul28;e2204287.?JMedVirol.2022Nov1.?NatMetab.2022Oct10.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YuweiHuang,etal.Migrasomeformationismediatedbyassemblyofmicron-scaletetraspaninmacrodomains.NatCellBiol.2019Aug;21(8):991-1002.[2].GotohK,etal.Theantitumoreffectsofmethyl-β-cyclodextrinagainstprimaryeffusionlymphomaviathedepletionofcholesterolfromlipidrafts.BiochemBiophysResCommun.2014Dec12;455(3-4):285-9.[3].TiwariG,etal.Cyclodextrinsindeliverysystems:Applications.JPharmBioalliedSci.2010Apr;2(2):72-9.[4].MundharaN,etal.Methyl-β-cyclodextrin,anactindepolymerizeraugmentstheantiproliferativepotentialofmicrotubule-targetingagents.SciRep.2019May21;9(1):7638.[5].ChenX,etal.Cholesteroldepletionfromtheplasmamembranetriggersligand-independentactivationoftheepidermalgrowthfactorreceptor.JBiolChem.2002Dec20;277(51):49631-7.[6].RodalSK,etal.Extractionofcholesterolwithmethyl-beta-cyclodextrinperturbsformationo
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