Phlorizin-Floridzin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPhlorizinCat.No.:HY-N0143CASNo.:60-81-1Synonyms:Floridzin;NSC2833分⼦式:C₂₁H₂₄O₁₀分⼦量:436.41作⽤靶点:SGLT;Na+/K+ATPase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:≥50mg/mL(114.57mM)H2O:1mg/mL(2.29mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2914mL11.4571mL22.9142mL5mM0.4583mL2.2914mL4.5828mL10mM0.2291mL1.1457mL2.2914mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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:≥2.5mg/mL(5.73mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.73mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.73mM);Clearsolution4.请依序添加每种溶剂：20%HP-β-CDinsalineSolubility:15.15mg/mL(34.72mM);Clearsolution;Needultrasonic5.请依序添加每种溶剂：PBSSolubility:1.75mg/mL(4.01mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY⽣物活性Phlorizin⼀种⾮选择性的SGLT抑制剂，对于hSGLT1和hSGLT2的Ki值分别为300和39nM。Phlorizin也⼀个Na+/K+-ATPase抑制剂。IC50&TargetSGLT1SGLT2体外研究Phlorizinisanon-selectiveSGLTinhibitorwithKisof300and39nMforhSGLT1andhSGLT2,respectively[1].PhlorizinisalsoaNa+/K+-ATPaseinhibitor[2].Phlorizinat2×10-4MinhibitsNa+andRb+-activatedATPaseactivitiesinhumanredcellmembranesby43%.At1mMand7mMRbCl,rubidiumuptakeisnotchangedorisslightlyinhibited(lessthan15%)by2×10-4MPhlorizin[2].CellviabilityisnotsignificantlyalteredbydosesofPhlorizin2levels.PhlorizindoesnotsuppressIL-6orTNF-αproduction,although100μMPhlorizincansignificantlyinhibitTNF-αexpression[3].体内研究PriortoPhlorizintreatment,thebloodglucoselevelinSDTfattyratsis370±49mg/dL.Sixhoursafterdosing,thebloodglucoselevelinthePhlorizintreatedgroupdecreasestoanalmostnormallevel(139±32mg/dL).Phlorizin-treatedSDTfattyratsareheavierthanvehicle-treatedSDTfattyratsafter12weeks.Phlorizintreatmentsignificantlydecreasesglucoseexcretionanddelaysinsulindecreases.CreatinineclearancedecreasessignificantlywithPhlorizintreatment.23weeksofPhlorizintreatmentpreventsthedecreaseofnervefibers(23.6±3.2fibers/mm).RetinalabnormalitiesarecompletelypreventedwithPhlorizin[4].PROTOCOLKinaseAssay[1]Resealedghostsareobtainedwiththeadditionof4×10-3MATPand5×10-3MMgCl2withorwithout5×10-4MPhlorizin(finalconcentration)whenredcellsarehemolyzed.Ghostscorrespondingto0.4-0.45mLoftheoriginalbloodcellsareincubatedwith0.9mLofMediumAand86RbClfor45or90minandtheradioactivityin200μLofthesupernatantisdetermined.TheATPaseactivityintheresealedghostsisdeterminedfromtheincreaseininorganicphosphateafterincubation[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellAssay[3]TheRAW264.7murinemacrophage-derivedcelllineisused.Cellviabilityismeasuredusingthe3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide(MTT)assay.Cells(105cells/well)areculturedin96-wellplatesandtreatedwithvaryingconcentrationsofPhlorizinfor24h.Next,thesupernatantisremovedandthecellsareincubatedwithMTT(50mg/mL)for4hat37°C.Theplatesarewashedandisopropanolisaddedtodissolveformazonecrystals,thentheabsorbancevaluesaremeasuredat570nmusingamicroplatereader[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalFemaleSDTfattyratsareusedinthisstudy.Atsixweeksofage,SDTfattyratsaredividedintotwogroupsAdministration[4](n=8);aPhlorizintreatedgroupandavehicletreatedgroup.Age-matchedfemaleSprague-Dawley(SD)ratsareusedascontrolanimals(n=8).Animalsarehousedinaclimate-controlledroom(temperature23±3°C,humidity55±15%,12hlightingcycle)andallowedfreeaccesstobasaldietandwater.Phlorizinisinjectedsubcutaneouslyoncedaily(100mg/kg/day)toanimalsinthePhlorizintreatedgroupfor23weeks.Twenty%propyleneglycolisadministeredtoanimalsinthevehicletreatedgroupandcontrolSDrats[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•CarbohydPolym.2021,118383.•Phytomedicine.2022Jul;101:154113.•VirusRes.2020Apr15;280:197901.•RSCAdv.20188:8469-8483.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PajorAM,etal.Inhibitorbindinginthehumanrenallow-andhigh-affinityNa+/glucosecotransporters.JPharmacolExpTher.2008Mar;324(3):985-91.[2].NakagawaA,etal.LocalizationofthephlorizinsiteonNa,K-ATPaseinredcellmembranes.JBiochem.1