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Medchemexpress/Apixaban(Synonyms: BMS-562247-01)/HY-50667/10mM*1mL in DMSO
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Medchemexpress/Apixaban(Synonyms: BMS-562247-01)/HY-50667/10mM*1mL in DMSO
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MedChemExpress
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HY-50667-10mM*1mLinDMSO
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Apixabanisahighlyselective,reversIBLeinhibitorofFactorXawithKiof0.08nMand0.17nMinhumanandrabbit,respectively.
Description

Apixabanisahighlyselective,reversibleinhibitorofFactorXawithKiof0.08nMand0.17nMinhumanandrabbit,respectively.

IC50&Target

IC50:0.08nM(HumanFactorXa),0.17nM(RabbitFactorXa)

InVitro

Apixabanexhibitsahighdegreeofpotency,selectivity,andefficacyonFactorXawithKiof0.08nMand0.17nMforHumanFactorXaandRabbitFactorXa,respectively[1].Invitro,Apixabanprolongstheclottingtimesofnormalhumanplasmawiththeconcentrations(EC2x)of3.6μM,0.37μM,7.4μM,and0.4μM,whicharerequiredrespectivelytodoubletheprothrombintime(PT),modifiedprothrombintime(mPT),activatedpartialthromboplastintime(APTT)andHepTest.Besides,Apixabanshowsthehighestpotencyinhumanandrabbitplasma,butlesspotencyinratanddogplasmainboththePTandAPTTassays[2].

InVivo

Apixabanshowstheexcellentpharmacokineticswithverylowclearance(Cl:0.02L/kg/h),andlowvolumeofdistribution(Vdss:0.2L/kg)inthedogs.Besides,Apixabanalsoexhibitsamoderatehalf-life(T1/2:5.8hours)andgoodoralbioavailABIlity(F:58%)[1].Inthearteriovenous-shuntthrombosis(AVST),venousthrombosis(VT)andelectricallymediatedcarotidarterialthrombosis(ECAT)rabbitmodels,Apixabanproducesdose-dependentantithromboticeffectswithEC50of270nM,110nMand70nM,respectively[2].ApixabansignificantlyinhibitsfactorXaactivitywithIC50of0.22μMinrabbitexvivo[3].Inchimpanzee,Apixabanalsoshowssmallvolumeofdistribution(Vdss:0.17L/kg),lowsystemicclearance(Cl:0.018L/kg/h),andgoodoralbioavailability(F:59%)[4].

ClinicalTrial
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References

  • [1].PintoDJ,etal.Discoveryof1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide(apixaban,BMS-562247),ahighlypotent,selective,efficacious,andorallybioavailableinhibitorofblo

    [2].WongPC,etal.Apixaban,anoral,directandhighlyselectivefactorXainhibitor:invitro,antithromboticandantihemostaticstudies.JThrombHaemost.2008May;6(5):820-9.

    [3].ZhangD,etal.Metabolism,pharmacokineticsandpharmacodynamicsofthefactorXainhibitorapixabaninrabbits.JThrombThrombolysis.2010Jan;29(1):70-80.

    [4].HeK,etal.Preclinicalpharmacokineticsandpharmacodynamicsofapixaban,apotentandselectivefactorXainhibitor.EurJDrugMetabPharmacokinet.2011Sep;36(3):129-39.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1763mL10.8814mL21.7628mL
5mM0.4353mL2.1763mL4.3526mL
10mM0.2176mL1.0881mL2.1763mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

PurifiedFXaisobtainedafteractivationwithRussell’svipervenomfollowedbyaffinitychromatography.TheresultingFXais>95%pureasjudgedbysodiumdodecylsulfatepolyacrylamidegelelectrophoresis.ThesubstrateaffinityvaluesforFXa,expressedastheMichaelis-Menten-Henriconstant(Km),forhuman,rabbit,ratanddogFXaaredeterminedusingthechromogenicsubstrateS-2765,andare36,60,240and70μM,respectively.Thesubstratehydrolysisismonitoredbymeasuringabsorbanceat405nmat25°Cforupto30minusingaSpectraMax384PlusplatereaderandSoftMax.FXaactivityforeachsubstrateandinhibitorconcentrationpairisdeterminedinduplicate.TheKivaluesarecalculatedbynon-linearleast-squaresfittingofthesteady-statesubstratehydrolysisratestotheequationforcompetitiveinhibition(Equation1)usingGRAFIT,wherevequalsreactionsvelocityinODmin−1,Vmaxequalsmaxiumumreactionvelocity,Sequalssubstrateconcentration,andIequalsinhibitorconcentration.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[2]

Apixabanisformulatedinvehicle(10%N,N-dimethylacetamide;30%1,2-propanediol;60%water).

Briefly,maleNewZealandWhiterabbitsareanesthetizedwithketamine(50mg/kgi.m.)andxylazine(10mg/kgi.m.),andtheirfemoralartery,jugularveinandfemoralveinarecatheterized.Theseanestheticsaresupplementedasneeded.Thrombosisisinducedbyanarteriovenous(AV)-shuntdevicecontainingasilkthread.BloodflowedfromthefemoralarteryviatheAVshuntintotheoppositefemoralveinfor40min.Theshuntisthendisconnectedandthesilkthreadcoveredwiththrombusisweighed.Asapixabanhasanoralbioavailabilityof<5%=""in=""rabbits=""(unpublished=""result),=""it=""is=""administered=""intravenously=""for=""in=""vivo=""studies.=""to=""achieve=""a=""stable=""plasma=""level=""with=""minimum=""experimental=""variability,=""apixaban,=""fondaparinux=""or=""vehicle=""is=""given=""by=""a=""continuous=""intravenous=""infusion=""1=""h=""prior=""to=""shunt=""placement.=""the=""infusion=""is=""continued=""throughout=""the=""experiment.=""warfarin=""or=""vehicle=""is=""dosed=""orally=""once=""daily=""for=""4=""days.=""on=""the=""fourth=""day=""after=""the=""last=""oral=""dose=""of=""warfarin=""or=""vehicle,=""rabbits=""are=""anesthetized=""1.5=""h=""later,=""and=""the=""treatment=""effect=""is=""evaluated=""about=""2=""h=""postdose.=""arterial=""blood=""samples=""for=""the=""determination=""of=""clotting=""times=""or=""plasma=""levels=""are=""collected=""20=""min=""after=""shunt=""placement.=""plasma=""levels=""of=""apixaban=""are=""measured=""by=""a=""specific=""and=""sensitive=""liquid=""chromatographic=""mass=""spectrometry=""method=""(lc/ms/ms).=""in=""rabbits=""treated=""with=""apixaban,=""fondaparinux=""or=""warfarin,=""the=""antithrombotic=""effects=""of=""these=""agents=""are=""expressed=""as=""percentage=""inhibition=""of=""thrombus=""formation=""based=""on=""the=""treated=""vs.=""the=""corresponding=""mean=""vehicle.=""the="">50value(dosethatproduced50%inhibitionofthrombusformation)isdeterminedasdescribedbelow.Theapixabangrouptreatmentconsistsofvehicle(10%N,N-dimethylacetamide;30%1,2-propanediol;60%water)(n=4),andapixaban(mg/kg/h)at0.03(n=7),0.1(n=7),0.3(n=7),1(n=7),and3(n=3).Thefondaparinuxgrouptreatmentconsistsofvehicle(saline)(n=6),andfondaparinux(mg/kg/h1)at0.01(n=5),0.03(n=5),0.1(n=5),0.3(n=5),and1(n=5).Thewarfaringrouptreatmentconsistsofvehicle(water)(n=6),andwarfarin(mg/kg/day)at0.1(n=6),0.3(n=6),1(n=6),and3(n=6).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].PintoDJ,etal.Discoveryof1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide(apixaban,BMS-562247),ahighlypotent,selective,efficacious,andorallybioavailableinhibitorofblo

    [2].WongPC,etal.Apixaban,anoral,directandhighlyselectivefactorXainhibitor:invitro,antithromboticandantihemostaticstudies.JThrombHaemost.2008May;6(5):820-9.

    [3].ZhangD,etal.Metabolism,pharmacokineticsandpharmacodynamicsofthefactorXainhibitorapixabaninrabbits.JThrombThrombolysis.2010Jan;29(1):70-80.

    [4].HeK,etal.Preclinicalpharmacokineticsandpharmacodynamicsofapixaban,apotentandselectivefactorXainhibitor.EurJDrugMetabPharmacokinet.2011Sep;36(3):129-39.

MolecularWeight

459.5

Formula

C₂₅H₂₅N₅O₄

CASNo.

503612-47-3

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:14.25mg/mL;H2O：<0.1="">

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

Purity:99.97%

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