Edoxaban tosylate Monohydrate

Catalog No.S5708 Synonyms: DU-176b tosylate Monohydrate

Edoxaban tosylate Monohydrate Chemical Structure

Molecular Weight(MW): 738.27

Edoxaban Tosylate is the tosylate salt form of edoxaban, an orally active inhibitor of factor Xa with anticoagulant activity.

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Biological Activity

Description Edoxaban Tosylate is the tosylate salt form of edoxaban, an orally active inhibitor of factor Xa with anticoagulant activity.
Targets
Factor Xa [1]
()
In vitro

In vitro bidirectional transport assays in human colon adenocarcinoma Caco-2 cell monolayers reveal that edoxaban is a substrate of the efflux transporter P-glycoprotein (P-gp) but is not a substrate for uptake transporters, such as organic anion-transporting polypeptide (OATP) 1B1, organic anion transporters (OATs) 1 and 3, or organic cation transporter (OCT) 2. Edoxaban has a minimal inhibitory effect on CYPs (IC50 ≥100 μM). It shows a weak inhibitory effect on P-gp, OATP1B1 and OATP1B3 (IC50 ≥50 μM), and a minimal effect on other drug transporters (OAT1, OAT3, OCT1 and OCT2; IC50≥100 μM)[3].

In vivo Edoxaban acts to selectively inhibit free factor Xa in the coagulation cascade, resulting in reduced thrombin generation and formation. Edoxaban is absorbed rapidly upon oral administration, providing peak plasma concentrations within one to two hours. The bioavailability of the tablet is 62%. Edoxaban can be taken without regard to meals, since food has not been shown to affect systemic exposure. Edoxaban is biphasic with a steady-state volume of distribution (Vdss) of 107 L. Edoxaban does not exhibit high protein binding (approximately 55% in vitro). Steady state is achieved within three days. In plasma, edoxaban primarily exists in its parent form and is minimally metabolized by hydrolysis or conjugation/ oxidation via CYP3A4. Edoxaban is primarily excreted unchanged in the urine. Renal clearance accounts for roughly half of the total clearance. The half-life of edoxaban is about 10 to 14 hours[2].

Protocol

Cell Research:

[4]

+ Expand
  • Cell lines: Caco-2 cell monolayers
  • Concentrations: 1-100 μM
  • Incubation Time: 2 hours
  • Method:

    --


    (Only for Reference)
Animal Research:

[5]

+ Expand
  • Animal Models: Male Apo E-deficient mice
  • Formulation: Methyl cellulose 400 solution (0.5% w/v)
  • Dosages: 15 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 49 mg/mL (66.37 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 738.27
Formula

C24H30ClN7O4S.C7H8O3S.H2O
 

CAS No. 1229194-11-9
Storage powder
in solvent
Synonyms DU-176b tosylate Monohydrate

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Factor Xa Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID