Encequidar-HM30181-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEncequidarCat.No.:HY-13646CASNo.:849675-66-7Synonyms:HM30181;HM30181A分⼦式:C₃₈H₃₆N₆O₇分⼦量:688.73作⽤靶点:P-glycoprotein作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:2.4mg/mL(3.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4519mL7.2597mL14.5195mL5mM---------10mM---------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。BIOLOGICALACTIVITY⽣物活性Encequidar(HM30181;HM30181A)⼀种有效的选择性的P-glycoprotein抑制剂。体外研究Encequidar(HM30181;HM30181A)isshowntobeapproximatelyequipotentwiththereferencePgpinhibitortariquidarininhibitingrhodamine123effluxfromCCRF-CEMTcells(IC50,tariquidar:8.2±2.0nM,1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEEncequidar(HM30181):13.1±2.3nM)[1].Encequidar(HM30181)showsahighselectivityformP-gpanditspotencyis20-50timeshigherthanthatoftariquitar,anotherthirdgenerationP-gpinhibitor[2].体内研究PETscanswiththePgpsubstrate(R)-[11C]NSC657799inFVBwild-typemicepretreatedi.v.withEncequidar(HM30181)(10or21mg/kg)failestoshowsignificantincreasesin(R)-[11C]NSC657799brainuptakecomparedwithvehicletreatedanimals[1].Encequidar(HM30181)inhibitsP-gpmainlyintheintestinalendothelium,whichcanbebeneficialbecausepan-inhibitionofP-gp,particularlyinthebrain,couldleadtodetrimentaladverseevents.Encequidar(HM30181)increasestheoralbioavailabilityofco-administeredNSC125973bymorethan12timesinrats[2].PROTOCOLAnimalMice[1]Administration[1]Encequidar(HM30181)mesylateisdissolvedin5%aqueousglucosesolution,containing20μL0.01Maq.HClandinjectedatavolumeof4mL/kg.FemaleFVBwild-typemice,aged8-12weeksweighing24±4gundergo(R)-[11C]NSC657799PETscanswithoutandwithi.v.pretreatmentwithcoldEncequidar(HM30181).Animalsareassignedto5groups(n=4pergroup).OnegroupispretreatedwithHM30181vehiclesolution(5%aq.glucosesolutioncontaining20μL0.01Maq.HCl)at60minbeforestartofthePETscan.Theothergroupsarepretreatedwitheither10mg/kgEncequidar(HM30181)at10,60or120minbeforePETorwith21mg/kgHM30181at10minbeforePET[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2021Jan12;12(1):312.•CritRevAnalChem.2021Mar10;1-15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BauerF,etal.InteractionofHM30181withP-glycoproteinatthemurineblood-brainbarrierassessedwithpositronemissiontomography.EurJPharmacol.2012Dec5;696(1-3):18-27.[2].KimTE,etal.EffectsofHM30181,aP-glycoproteininhibitor,onthepharmacokineticsandpharmacodynamicsofloperamideinhealthyvolunteers.BrJClinPharmacol.2014Sep;78(3):556-64.McePdfHeightCaution:Producthasnotbeenfullyvalidated