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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Rivaroxaban(Synonyms: BAY 59-7939)/HY-50903/10mM*1mL in DMSO
商品详细Medchemexpress/Rivaroxaban(Synonyms: BAY 59-7939)/HY-50903/10mM*1mL in DMSO
Medchemexpress/Rivaroxaban(Synonyms: BAY 59-7939)/HY-50903/10mM*1mL in DMSO
Medchemexpress/Rivaroxaban(Synonyms: BAY 59-7939)/HY-50903/10mM*1mL in DMSO
商品编号： HY-50903-10mM*1mLinDMSO
品牌： MedChemExp
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产地： 美国(厂家直采)
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产品分类： 小分子
公司分类： Small_molecule
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商品介绍
Rivaroxabanisahighlypotentandselective,directFactorXa(FXa)inhibitor,achievingastronggaininanti-FXapotency(IC500.7nM;Ki0.4nM).
Description

Rivaroxabanisahighlypotentandselective,directFactorXa(FXa)inhibitor,achievingastronggaininanti-FXapotency(IC500.7nM;Ki0.4nM).

IC50&Target

IC50:0.7nM(FXa)[1]
Ki:0.4nM(FXa)[1]

InVitro

Rivaroxaban(BAY59-7939)isanoral,directFactorXa(FXa)inhibitorindevelopmentforthepreventionandtreatmentofarterialandvenousthrombosis.RivaroxabancompetitivelyinhibitshumanFXa(Ki0.4nM)with>10000-foldgreaterselectivitythanforotherserineproteases;italsoinhibitsprothrombinaseactivity(IC502.1nM).RivaroxabaninhibitsendogenousFXamorepotentlyinhumanandrabbitplasma(IC5021nM)thanratplasma(IC50290nM).Itdemonstratesanticoagulanteffectsinhumanplasma,doublingprothrombintime(PT)andactivatespartialthromboplastintimeat0.23and0.69μM,respectively[2].

InVivo

Rivaroxaban(BAY59-7939)isapotentandselective,directFXainhibitorwithexcellentinvivoactivityandgoodoralbioavailABIlity[1].Rivaroxaban(BAY59-7939),admiNISTeredbyi.v.bolusbeforethrombusinduction,reducesthrombusformation(ED500.1mg/kg),inhibitsFXa,andprolongsPTdosedependently.PTandFXaareaffectedslightlyattheED50(1.8-foldincreaseand32%inhibition,respectively).At0.3mg/kg(doseleADIngtoalmostcompleteinhibitionofthrombusformation),RivaroxabanmoderatelyprolongsPT(3.2±0.5-fold)andinhibitsFXaactivity(65±3%)[2].

ClinicalTrial
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References

  • [1].RoehrigS,etal.Discoveryofthenovelantithromboticagent5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide(BAY59-7939):anoral,directfactorXainhibitor.JMedChem.2005Sep22;48(19)

    [2].PerzbornE,etal.InvitroandinvivostudiesofthenovelantithromboticagentBAY59-7939--anoral,directFactorXainhibitor.JThrombHaemost.2005Mar;3(3):514-21.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.2942mL11.4710mL22.9421mL
5mM0.4588mL2.2942mL4.5884mL
10mM0.2294mL1.1471mL2.2942mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

TheactivityofRivaroxaban(BAY59-7939)againstpurifiedserineproteasesismeasuredusingchromogenicorfluorogenicsubstratesin96-wellmicrotiterplatesat25°C.TheenzymesareincubatedwithRivaroxabanoritssolvent,DMSO,for10min.Thereactionsareinitiatedbytheadditionofthesubstrate,andthecolororfluorescenceismonitoredcontinuouslyat405nmusingaSpectraRainbowThermoReader,orat630/465nmusingaSPECTRAfluorplus,respectively,for20min.Enzymaticactivityisanalyzedinthefollowingbuffers(finalconcentrations):humanFXa(0.5nM),rabbitFXa(2nM),ratFXa(10nM),orurokinase(4nM)in50mMTris-HClbuffer,pH8.3,150mMNaCl,and0.1%bovineserumalbumin(BSA);PefachromeFXa(50-800μM)orchromozymU(250μM)withthrombin(0.69nM),trypsin(2.2nM),orplasmin(3.2nM)in0.1μMTris-HCl,pH8.0,and20mMCaCl2;chromozymTH(200μM),chromozymplasmin(500μM),orchromozymtrypsin(500μM)withFXIa(1nM)orAPC(10nM)in50mMphosphatebuffer,pH7.4,150mMNaCl;andS2366(150or500μM)withFVIIa(1nM)andtissuefactor(3nM)in50mMTris-HClbuffer,pH8.0,100mMNaCl,5mMCaCl2and0.3%BSA,H-D-Phe-Pro-Arg-6-amino-1-naphthalene-benzylsulfon-amideH2O(100μM)andmeasuredfor3h.TheFIXab/FXassay,comprisingFIXab(8.8nM)andFX(9.5nM)in50mMTris-HClbuffer,pH7.4,100mMNaCl,5mMCaCl2and0.1%BSA,isstartedbytheadditionofI-1100(50μM),andmeasuredfor60min.Theinhibitoryconstant(Ki)againstFXaiscalculatedaccordingtotheCheng-Prusoffequation(Ki=IC50/1+[S]/Km),where[S]isthesubstrateconcentration,andKmistheMichaelis-Mentenconstant.KmisdeterminedfromaLineweaver-Burkplot.TheIC50istheamountofinhibitorrequiredtodiminishtheinitialvelocityofthecontrolby50%[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2]

Rivaroxaban(BAY59-7939)isdissolvedinpolyethyleneglycol/H2O/glycerol(Rat)[2].

Rat[2]
Fasted,maleWistarrats(HsdCpb:WU)areused.RatvenousstasismodelThrombusformationisinducedinanesthetizedrats(n=10perdosegroup),withminormodifications.TheaBDominalvenacavaisexposedandtwoloosesutures(8-10mmapart)areplacedbelowtheleftrenalvenousbranch.Rivaroxabandissolvedinpolyethyleneglycol/H2O/glycerol(996g/100g/60g),orvehicleisgivenbyintravenous(i.v.)bolusinjectionintoatailvein15minbeforethrombusinduction.Thromboplastin(0.5mg/kg)isinjectedintoafemoralveinand,after15s,theproximalanddistalsuturesaretied.Fifteenminuteslater,theligatedsegmentisremoved,thethrombuswithdrawnandweighed.Bloodsamplesareobtainedbycardiacpunctureimmediatelybeforethrombusremoval.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].RoehrigS,etal.Discoveryofthenovelantithromboticagent5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide(BAY59-7939):anoral,directfactorXainhibitor.JMedChem.2005Sep22;48(19)

    [2].PerzbornE,etal.InvitroandinvivostudiesofthenovelantithromboticagentBAY59-7939--anoral,directFactorXainhibitor.JThrombHaemost.2005Mar;3(3):514-21.

MolecularWeight

435.88

Formula

C₁₉H₁₈ClN₃O₅S

CASNo.

366789-02-8

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.96%