| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
When taken orally, darexaban, an inhibitor of factor Xa (FXa), is quickly and thoroughly metabolized to produce its glucuronide conjugate, YM-222714. In addition to inhibiting prothrombin activation caused by the prothrombinase complex or entire blood clots with potency comparable to that of free FXa, darexaban also specifically and competitively inhibits human FXa [2].
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| ln Vivo |
In mice, Darexaban decreased FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban 3 mg/kg can extend prothrombin time (PT) [2]. In a mouse model of pulmonary thromboembolism (PE), darexaban dosage-dependently reduced mortality, with a substantial impact at a dose of 10 mg/kg [2]. In a mouse model of FeCl3-induced venous thrombosis (VT), Darexaban (0.3-10 mg/kg) dose-dependently reduced thromboprotein content, with significant effects at doses of 3 mg/kg or higher [2].
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| References |
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| Additional Infomation |
Darexaban has been used in trials studying the prevention and basic science of Japanese, Caucasian, Thromboembolism, Pharmacodynamics, and Pharmacokinetics, among others.
Tanexaban is an orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Tanexaban is extensively metabolized in the liver to its active metabolite and is excreted by the kidneys and in the feces. |
| Molecular Formula |
C27H30N4O4
|
|---|---|
| Molecular Weight |
474.5515
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| Exact Mass |
474.227
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| CAS # |
365462-23-3
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| PubChem CID |
9912771
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.196
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
691
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IJNIQYINMSGIPS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30N4O4/c1-30-15-4-16-31(18-17-30)21-11-7-19(8-12-21)27(34)29-25-23(5-3-6-24(25)32)28-26(33)20-9-13-22(35-2)14-10-20/h3,5-14,32H,4,15-18H2,1-2H3,(H,28,33)(H,29,34)
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| Chemical Name |
N-[2-hydroxy-6-[(4-methoxybenzoyl)amino]phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~526.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01405989 | Completed | Drug: darexaban Drug: ketoconazole |
Pharmacokinetics of Darexaban and Metabolites |
Astellas Pharma Inc | January 2010 | Phase 1 |
| NCT01406002 | Completed | Drug: darexaban Drug: Rifampicin |
Pharmacokinetics of Darexaban and Metabolites |
Astellas Pharma Inc | January 2010 | Phase 1 |
| NCT01514825 | Completed | Drug: YM150 Drug: Placebo |
Healthy Elderly Subject Pharmacokinetic of YM150 |
Astellas Pharma Inc | November 2006 | Phase 1 |
| NCT01424332 | Completed | Drug: Darexaban Drug: Acetyl Salicylic Acid (ASA) |
Pharmacodynamic and Pharmacokinetic Interaction |
Astellas Pharma Inc | December 2007 | Phase 1 |
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