Edoxaban tosylate Monohydrate
Catalog No.S5708 Synonyms: DU-176b tosylate Monohydrate
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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|Description||Edoxaban Tosylate is the tosylate salt form of edoxaban, an orally active inhibitor of factor Xa with anticoagulant activity.|
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).
|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.|
-  Honda Y, et al. Thromb Res. 2016, 141:17-21.
-  Lewey Chan, et al. P T. 2015 Oct; 40(10): 651-655, 695.
-  Dolly A. Parasrampuria, et al. Clin Pharmacokinet. 2016, 55: 641–655.
|In vitro||DMSO||49 mg/mL (66.37 mM)|
* 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.
|Synonyms||DU-176b tosylate Monohydrate|
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