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Edoxaban

SKU: orb1305585

Description

Edoxaban (Lixiana, DU-176b) is a potent, selective, and orally active direct inhibitor of coagulation factor Xa (FXa), exhibiting over 10,000-fold selectivity versus related serine proteases. This small molecule anticoagulant is widely used in research for investigating thrombosis, stroke prevention, and its pharmacological effects in both in vitro enzymatic assays and in vivo disease models.

Research Area

Metabolism Research, Protein Biochemistry

Images & Validation

Key Properties

CAS Number480449-70-5
MW548.06
Purity99.71% (May vary between batches)
FormulaC24H30ClN7O4S
SMILESN(C(=O)C1=NC2=C(S1)CN(C)CC2)[C@H]3[C@@H](NC(C(NC4=CC=C(Cl)C=N4)=O)=O)CC[C@H](C(N(C)C)=O)C3
TargetThrombin,Factor Xa
SolubilityDMSO:2.74 mg/mL (5 mM)

Bioactivity

In Vivo
Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) inhibits thrombus formation in rat thrombosis models in a dose-dependent manner . Animal Model: Wistar rats (210-240 g) with venous stasis thrombosis model Dosage: 0.5 mg/kg, 2.5 mg/kg, 12.5 mg/kg Administration: Oral administration Result: Dose-dependently inhibited thrombus formation in rat thrombosis models.
In Vitro
Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with K i values of 6.90 nM, 0.715 nM and 0.457 nM, respectively . Prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT) of human plasma are prolonged by Edoxaban (DU-176b) in a concentration-dependent way, doubling PT and APTT at 0.256 and 0.508 μM, respectively. The double clotting time (CT2) for TT, however, was much higher (4.95 μM), reflecting its anti-thrombin activity. Thrombin-induced platelet aggregation is inhibited by a high concentration of Edoxaban (DU-176b) (IC 50 : 2.90 μM), reflecting its weak anti-thrombin activity . Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein .

Storage & Handling

Storagekeep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Lixiana, Edoxaban, FactorXa, Factor Xa, Thrombin

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Key Properties

No computed properties available.

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Edoxaban (orb1305585)

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5 mg
$ 90.00
10 mg
$ 110.00
25 mg
$ 140.00
50 mg
$ 160.00
100 mg
$ 210.00
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