Phlorizin-Floridzin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPhlorizinCat.No.:HY-N0143CASNo.:60-81-1Synonyms:Floridzin;NSC2833分?式:C??H??O??分?量:436.41作?靶點(diǎn):SGLT;Na+/K+ATPase作?通路:MembraneTransporter/IonChannel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:≥50mg/mL(114.57mM)H2O:1mg/mL(2.29mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2914mL11.4571mL22.9142mL5mM0.4583mL2.2914mL4.5828mL10mM0.2291mL1.1457mL2.2914mL請根據(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?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?；如在配制過程中出現(xiàn)沉淀1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.73mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.73mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.73mM);Clearsolution4.請依序添加每種溶劑：20%HP-β-CDinsalineSolubility:15.15mg/mL(34.72mM);Clearsolution;Needultrasonic5.請依序添加每種溶劑：PBSSolubility:1.75mg/mL(4.01mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性Phlorizin?種?選擇性的SGLT抑制劑，對(duì)于hSGLT1和hSGLT2的Ki值分別為300和39nM。Phlorizin也?個(gè)Na+/K+-ATPase抑制劑。IC50&TargetSGLT1SGLT2體外研究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].體內(nèi)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?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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