Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEncequidarmesylateCat.No.:HY-13646ACASNo.:849675-87-2Synonyms:HM30181mesylate;HM30181Amesylate分?式:C??H??N?O??S分?量:784.83作?靶點:P-glycoprotein作?通路:MembraneTransporter/IonChannel儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗DMSO:25mg/mL(31.85mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.2742mL6.3708mL12.7416mL5mM0.2548mL1.2742mL2.5483mL10mM0.1274mL0.6371mL1.2742mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(3.19mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Encequidarmesylate(HM30181mesylate;HM30181Amesylate)P-糖蛋?(P-glycoprotein)的有效競爭性抑制劑。IC50&TargetP-glycoprotein[1][2].體外研究Treatmentof0.1or1nMEncequidar(HM30181)leadto20and42%inhibitionofsurvivalatthe100nMand1000nMNSC125973treatment,respectively[2].體內研究TheplasmaconcentrationsofEncequidar(HM30181)arehigherforthesimultaneousadministrationwiththemicrocapsulethanwiththepowder;providingsignificantdifferencesfrom1to2h.Themicrocapsulehasabouta1.7-foldfasterTmaxanda1.6-foldhigherAUCvaluecomparedwiththepowder(2.5±0.6vs.4.3±0.9h;107.7±20.1vs.64.3±18.0hng/mL).ThefasterandoverallimprovedabsorptionofEncequidar(HM30181)inmicrocapsuleformmightbeduetotheremarkableenhancementoftheaqueoussolubilityanddissolutionresultingfromitscrystallineconversiontotheamorphousformandparticlesizereduction[1].PROTOCOLAnimalRats[1]Administration[1]Thecannulisedratsaredividedintofourgroups,eachcomprisesof6rats.Encequidar(HM30181)powderorEncequidar(HM30181)-loadedmicrocapsulesareenclosedinhardcapsules.OnegroupofratsisdosedorallywithNSC125973solutiononly,atadrugdoseof20mg/kg.TheratsintheothertwogroupsareadministeredNSC125973solutionatadrugdoseof20mg/kgsimultaneouslywitheithercapsulescontainingEncequidar(HM30181)powderormicrocapsules(equivalentto20mg/kgEncequidar(HM30181))[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?NatCommun.2021Jan12;12(1):312.?CritRevAnalChem.2021Mar10;1-15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KimJC,etal.EffectofHM30181mesylatesalt-loadedmicrocapsulesontheoralabsorptionofNSC125973asanovelP-glycoproteininhibitor.IntJPharm.2016Jun15;506(1-2):93-101.[2].JooKM,etal.ResponseofbrainspecificmicroenvironmenttoP-glycoproteininhibitor:animportantfactordeterminingtherapeuticeffectofP-glycoproteininhibitoronbrainmetastatictumors.IntJOncol.2008Oct;33(4):705-12.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenf