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Darexaban

Catalog No. T31206   CAS 365462-23-3
Synonyms: YM 150, Darexaban, Tanexaban, YM150

Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.

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Darexaban Chemical Structure
Darexaban, CAS 365462-23-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
2 mg In stock $ 57.00
5 mg In stock $ 87.00
10 mg In stock $ 147.00
25 mg In stock $ 296.00
50 mg In stock $ 482.00
100 mg In stock $ 689.00
1 mL * 10 mM (in DMSO) In stock $ 93.00
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Purity: 98.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.
Targets&IC50 FXa:54.6 nM
Synonyms YM 150, Darexaban, Tanexaban, YM150
Molecular Weight 474.55
Formula C27H30N4O4
CAS No. 365462-23-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 245 mg/mL (516.28 mM)

TargetMolReferences and Literature

1. Lip GY, Halperin JL, Petersen P, Rodgers GM, Pall D, Renfurm RW. A Phase II, double-blind, randomized, parallel group, dose-finding study of the safety and tolerability of darexaban compared with warfarin in patients with non-valvular atrial fibrillation: the oral factor Xa inhibitor for prophylaxis of stroke in atrial fibrillation study 2 (OPAL-2). J Thromb Haemost. 2015 Aug;13(8):1405-1doi: 10.1111/jth.1302Epub 2015 Jul 1 2. Eriksson BI, Agnelli G, Gallus AS, Lassen MR, Prins MH, Renfurm RW, Kashiwa M, Turpie AG. Darexaban (YM150) versus enoxaparin for the prevention of venous thromboembolism after total hip arthroplasty: a randomised phase IIb dose confirmation study (ONYX-3). Thromb Haemost. 2014 Feb;111(2):213-2doi: 10.1160/TH13-04-0296. Epub 2013 Oct 17. PubMed PMID: 24136153. 3. Kadokura T, Kashiwa M, Groenendaal D, Heeringa M, Mol R, Verheggen F, Garcia-Hernandez A, Onkels H. Clinical pharmacokinetics, pharmacodynamics, safety and tolerability of darexaban, an oral direct factor Xa inhibitor, in healthy Caucasian and Japanese subjects. Biopharm Drug Dispos. 2013 Nov;34(8):431-4doi: 10.1002/bdd.1858. Epub 2013 Sep 20. PubMed PMID: 23929659. 4. Kadokura T, Groenendaal D, Heeringa M, Mol R, Verheggen F, Garcia-Hernandez A, Onkels H. Darexaban (YM150), an oral direct factor Xa inhibitor, has no effect on the pharmacokinetics of digoxin. Eur J Drug Metab Pharmacokinet. 2014 Mar;39(1):1-9. doi: 10.1007/s13318-013-0141-Epub 2013 Jun 1PubMed PMID: 23754514.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Drug Repurposing Compound Library ReFRAME Related Library Orally Active Compound Library Human Metabolite Library Clinical Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Darexaban 365462-23-3 Metabolism Factor Xa Serine endopeptidases time YM-150 YM 150 Ser/Thr Protease Fxa oral antithrombotic Inhibitor prothrombin Serine proteases Threonine proteases Darexaban, Tanexaban anticoagulant YM150 inhibit inhibitor

 

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