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Cat. No. Name Size Price Add Cart
KI3500EdoxabanQuoteQuote

Chemical Characteristic

Product NameEdoxaban
SynonymsDU-176b
CAS No.480449-70-5
Molecular Weight 548.06
FormulaC24H30ClN7O4S
Chemical NameEthanediamide, 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
SmilesC(=O)(C(=O)Nc1ccc(cn1)Cl)NC1[C@@H](C[C@H](CC1)C(=O)N(C)C)NC(=O)c1sc2CN(CCc2n1)C
Chemical Structure

Biological activities

Edoxaban is an oral and direct factor Xa inhibitor. Edoxaban inhibits human free factor Xa with a Ki value of 0.561 nM. Edoxaban also inhibits factor Xa bound to the prothrombinase complex with a Ki value of 2.98 nM. In addition, edoxaban exhibits>10 000-fold selectivity for factor Xa relative to thrombin and has no inhibitory effects on other biologically relevant serine proteases.[1] In human liver microsomes (HLM), edoxaban is NADPH-dependently metabolized to M-5 (N-oxidation of thiazolopyridine ring), M-6 (oxidative Ndemethylation of thiazolopyridine ring), and M-7 (hydroxylated metabolite at the N,N-dimethylcarbamoyl group of edoxaban, putative metabolite).[2] In human plasma, edoxaban doubles prothrombin time and activates partial thromboplastin time at concentrations of 256 and 508 nM, respectively. In vivo, edoxaban is highly absorbed in rats and monkeys. In rats, edoxaban at the concentrations of 2.5 and 5 mg/kg produces significant inhibition of factor Xa activity in plasma by 86%and 94%inhibition, respectively. Similarly, in cynomolgus monkeys, edoxaban treatment leads to a rapid onset of anti-factor Xa activity. In addition, edoxaban also dose-dependently inhibits thrombus formation in rat and rabbit thrombosis models in vivo.[1] Moreover, edoxaban at a supratherapeutic dose (1 mg/kg intravenously) significantly prolongs bleeding time and prothrombin time (PT), and also inhibits thrombin generation in the rat model of template bleeding.[3]

Protocols

In vitro, Prior to use, edoxaban is dissolved in DMSO.[4]

References

[1] Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008, 6(9): 1542-1549.
[2] H. Masumoto, et al. In vitroMetabolism of Edoxaban and the Enzymes Involved in the Oxidative Metabolism of Edoxaban. American Association of Pharmaceutical Scientists. 2010.
[3] Camm AJ, et al. Edoxaban: a new oral direct factor xa inhibitor. Drugs. 2011, 71(12): 1503-1526.
[4] Samama MM, et al. In vitro study of the anticoagulant effects of edoxaban and its effect on thrombin generation in comparison to fondaparinux. Thromb Res. 2012, 129(4): e77-e82.

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