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MedKoo Biosciences/Edoxaban tosylate monohydrate/314259/200mg

Edoxaban(INN,codenamedDU-176b,tradenameLixiana)isapotent,selectivefactorXainhibitor,whichhasgoodoralbioavailABIlity.EdoxabanisananticoagulantdrugwhichactsasadirectfactorXainhibitor.ItisbeingdevelopedbyDaiichiSankyo.ItwasapprovedinJuly2011inJapanforpreventionofvenousthromboembolisms(VTE)followinglower-limborthopedicsurgery.ItwasalsoapprovedbytheFDAinJanuary2015forthepreventionofstrokeandnon–central-nervous-systemsystemicembolism.

MedKooCat#:314259
Name:Edoxabantosylatemonohydrate
CAS#:1229194-11-9(tosylatehydrate)
ChemicalFormula:C31H40ClN7O8S2
ExactMass:
MolecularWeight:738.272
ElementalAnalysis:C,50.43;H,5.46;Cl,4.80;N,13.28;O,17.34;S,8.69


Synonym:DU176b;DU-176b;DU176b;Edoxaban;Edoxabantosylatemonohydrate,tradenameLixiana.

IUPAC/ChemicalName:N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-(dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)cyclohexyl)oxalamide4-methylbenzenesulfonatehydrate

InChiKey:PSMMNJNZVZZNOI-SJILXJHISA-N

InChiCode:InChI=1S/C24H30ClN7O4S.C7H8O3S.H2O/c1-31(2)24(36)13-4-6-15(27-20(33)21(34)30-19-7-5-14(25)11-26-19)17(10-13)28-22(35)23-29-16-8-9-32(3)12-18(16)37-23;1-6-2-4-7(5-3-6)11(8,9)10;/h5,7,11,13,15,17H,4,6,8-10,12H2,1-3H3,(H,27,33)(H,28,35)(H,26,30,34);2-5H,1H3,(H,8,9,10);1H2/t13-,15-,17+;;/m0../s1

SMILESCode:O=C(NC1=NC=C(Cl)C=C1)C(N[C@@H]2[C@H](NC(C(S3)=NC4=C3CN(C)CC4)=O)C[C@@H](C(N(C)C)=O)CC2)=O.CC5=CC=C(S(=O)(O)=O)C=C5.[H]O[H]


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:
Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:
SolubleinDMSO.

ShelfLife:
>2yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:
0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:
293490


AdditionalInformation

RelatedCAS#
1229194-11-9(Edoxabantosylatehydrate);
480449-70-5(Edoxabanfreebase).


References

1:TraynorK.Edoxabanapprovedforembolismprevention.AmJHealthSystPharm.2015Feb15;72(4):258.doi:10.2146/news150011.PubMedPMID:25631826.

2:MarluR,PolackB,PernodG.Exvivoreversaloftheanticoagulanteffectsofedoxaban-commentsonthestudybyHalimetal.ThrombRes.2015Jan7.pii:S0049-3848(15)00004-3.doi:10.1016/j.thromres.2015.01.002.[Epubaheadofprint]PubMedPMID:25628140.

3:DeCaterinaR.[Clinicalimplicationsofedoxabaninthecurrentscenariooforalanticoagulants].GItalCardiol(Rome).2014Dec;15(12):27-9.doi:10.1714/1744.18990.Italian.PubMedPMID:25621575.

4:DiPasqualeG,RivaL.[Edoxabanforthetreatmentofatrialfibrillation:theENGAGEAF-TIMI48study].GItalCardiol(Rome).2014Dec;15(12):22-6.doi:10.1714/1744.18988.Italian.PubMedPMID:25621574.

5:AndreottiF.[Molecularstructureandpharmacologyofedoxaban].GItalCardiol(Rome).2014Dec;15(12):11-6.doi:10.1714/1744.18984.Italian.PubMedPMID:25621572.

6:MorishimaY,KamisatoC.Laboratorymeasurementsoftheoraldirectfactorxainhibitoredoxaban:comparisonofprothrombintime,activatedpartialthromboplastintime,andthrombingenerationassay.AmJClinPathol.2015Feb;143(2):241-7.doi:10.1309/AJCPQ2NJD3PXFTUG.PubMedPMID:25596250.

7:ParasrampuriaDA,MarburyT,MatsushimaN,ChenS,WickremasinghaPK,HeL,DishyV,BrownKS.Pharmacokinetics,safety,andtolerabilityofedoxabaninend-stagerenaldiseasesubjectsundergoinghaemodialysis.ThrombHaemost.2015Jan8;113(3).[Epubaheadofprint]PubMedPMID:25566930.

8:SpanosK,GiannoukasAD.Re:'Kakkosetal.EfficacyandSafetyoftheNewOralAnticoagulantsDabigatran,Rivaroxaban,Apixaban,andEdoxabanintheTreatmentandSecondaryPreventionofVenousThromboembolism:ASystematicReviewandMeta-analysisofPhaseIIITrials'.EurJVascEndovascSurg.2014Dec30.pii:S1078-5884(14)00655-8.doi:10.1016/j.ejvs.2014.11.019.[Epubaheadofprint]PubMedPMID:25556084.

9:KakkosSK,KirkilesisGI,TsolakisIA.Responseto'Re:Kakkosetal.EfficacyandSafetyoftheNewOralAnticoagulantsDabigatran,Rivaroxaban,Apixaban,andEdoxabanintheTreatmentandSecondaryPreventionofVenousThromboembolism:ASystematicReviewandMeta-analysisofPhaseIIITrials'.EurJVascEndovascSurg.2014Dec30.pii:S1078-5884(14)00656-X.doi:10.1016/j.ejvs.2014.12.007.[Epubaheadofprint]PubMedPMID:25556083.

10:HerzogE,KaspereitF,KregeW,DoerrB,Mueller-CohrsJ,PragstI,MorishimaY,DickneiteG.EffectiveReversalofEdoxaban-associatedBleedingwithFour-factorProthrombinComplexConcentrateinaRabbitModelofAcuteHemorrhage.Anesthesiology.2015Feb;122(2):387-98.doi:10.1097/ALN.0000000000000520.PubMedPMID:25419685.

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