VIT-2763-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVIT-2763Cat.No.:HY-112220CASNo.:2095668-10-1分⼦式:C₂₁H₂₁FN₆O₂分⼦量:408.43作⽤靶点:Ferroportin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:125mg/mL(306.05mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4484mL12.2420mL24.4840mL5mM0.4897mL2.4484mL4.8968mL10mM0.2448mL1.2242mL2.4484mL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、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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.09mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.09mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性VIT-2763具有⼝服活性的铁转运蛋⽩(ferroportin)的抑制剂，抑制hepcidin与铁转运蛋⽩结合，阻滞铁外流。VIT-2763有⽤于地中海贫⾎症的潜⼒。体外研究VIT-2763dosedependentlyreducesthefluorescencepolarizationsignal,indicatingthatVIT-2763displacesTMR-hepcidinfromferroportin(IC50of24±13nM)[1].VIT-2763inducesBLAreportergeneactivitywithanaverageEC50of140±50nM,asaconsequenceofincreasingintracellularironconcentrationscausedbyblockedironexportinHEK293cells[1].VIT-2763(100nM)triggersubiquitinationandsubsequentinternalizationanddegradationofferroportin[1].CellViabilityAssay[1].CellLine:J774cells.Concentration:100nM.IncubationTime:10,20,40,60,or120minutes.Result:Inducedferroportininternalizationandubiquitination.体内研究VIT-2763(30,100mg/kg,orallytwicedailyfor36days)decreasesserumironandpreventedliverironloadinginHbbth3/+mice[1].VIT-2763didnotchangethetotalliveriron[1].VIT-2763(30,100mg/kg,orallytwicedailyfor36days)significantlycorrectsanemiaandimprovedRBCparametersinHbbth3/+mice.VIT-2763decreasesthepercentageofROS-positiveRBCsinHbbth3/+micefrom67%to30%[1].VIT-2763decreasesapoptosisandextendsthelifespanofRBCsinHbbth3/+mice[1].AnimalModel:Hbbth3/+mice[1].Dosage:30,100mg/kg.Administration:Orallytwicedailyfor36days.Result:Significantlydecreasedserumironlevelsby77%(30mg/kg)and84%(100mg/kg),SignificantlyincreasedHblevels(asofday8oftreatment),RBCcounts,meancorpuscularHbconcentration(MCHC),andsignificantlyloweredreticulocytecounts,meancorpuscularHb(MCH),meancorpuscularvolume(MCV),andRBCdistributionwidth(RDW)inHbbth3/+mice,ascomparedwiththeHbbth3/+vehiclegroup.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].VaniaManolova,etal.OralFerroportinInhibitorAmelioratesIneffectiveErythropoiesisinaModelofβ-Thalassemia.JClinInvest.2019Dec9;130(1):491-506.McePdfHeightCaution:Producthasnotbeenfullyvalidated