1. Metabolic Enzyme/Protease
  2. Factor Xa
  3. Darexaban

Darexaban (Synonyms: YM150)

Cat. No.: HY-14853
Handling Instructions

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.

For research use only. We do not sell to patients.

Darexaban Chemical Structure

Darexaban Chemical Structure

CAS No. : 365462-23-3

Size Price Stock Quantity
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects[1][2][3].

In Vitro

Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In mice, Darexaban inhibits FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg[2].
In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg[2].
In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

474.55

Formula

C₂₇H₃₀N₄O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (526.81 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1073 mL 10.5363 mL 21.0726 mL
5 mM 0.4215 mL 2.1073 mL 4.2145 mL
10 mM 0.2107 mL 1.0536 mL 2.1073 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Darexaban
Cat. No.:
HY-14853
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