Edoxaban tosylate monohydrate

Research use only, not for human use.

A potent and orally active Factor Xa inhibitor with Ki of 0.561 nM; also inhibits prothrombinase (Ki=2.98 nM).

A potent and orally active Factor Xa inhibitor with Ki of 0.561 nM; also inhibits prothrombinase (Ki=2.98 nM), weakly inhibits thrombin and FIXa (Ki=6.0 uM, and 41.7 uM); exhibits >10,000-fold selectivity for Fxa over FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin and chymotrypsin; inhibits thrombus formation in rat and rabbit thrombosis models.Thrombosis Approved(In Vitro):Edoxaban monohydrate (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner.Edoxaban monohydrate inhibits thrombin-induced platelet aggregation, with an IC50 of 2.90 μM.(In Vivo):Edoxaban monohydrate (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT.

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Animal Model:Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model).Dosage:0.5, 2.5 and 12.5 mg/kg Administration:Oral administration; once Result:Inhibited exogenous FXa activity.

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Metabolic Enzyme/Protease

Factor Xa

FactorXa|Thrombin

Cardiovascular Disease

Thrombosis

1229194-11-9

738.2744

C31H40ClN7O8S2

>98% (HPLC)

10 mM in DMSO

CC1=CC=C(C=C1)S(=O)(=O)O.CN1CCC2=C(C1)SC(=N2)C(=O)N[C@@H]3C[C@H](CC[C@@H]3NC(=O)C(=O)NC4=NC=C(C=C4)Cl)C(=O)N(C)C.O

Ethanediamide, N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]-, 4-methylbenzenesulfonate, hydrate (1:1:1)

(-20℃)

With Ice Pack

≥ 2 years