Darexaban

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].

Product Specifications

CAS Number

[365462-23-3]

Product Name Alternative

YM150

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Factor Xa; Ser/Thr Protease

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/darexaban.html

Purity

98.05

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(NC1=C(NC(C2=CC=C(OC)C=C2)=O)C=CC=C1O)C3=CC=C(N4CCN(C)CCC4)C=C3

Molecular Formula

C27H30N4O4

Molecular Weight

474.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Fukushi Hirayama, et al. Discovery of N-[2-hydroxy-6- (4-methoxybenzamido) phenyl]-4- (4-methyl-1,4-diazepan-1-yl) benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. J Med Chem. 2011 Dec 8;54 (23) :8051-65.|[2]Seiji Kaku, et al. Darexaban: anticoagulant effects in mice and human plasma in vitro, antithrombotic effects in thrombosis and bleeding models in mice and effects of anti-inhibitor coagulant complex and recombinant factor VIIa. Thromb Res. 2013 May;131 (5) :450-6.|[3]Milan Remko, et al. Theoretical Study of Molecular Structure and Physicochemical Properties of Novel Factor Xa Inhibitors and Dual Factor Xa and Factor IIa Inhibitors. Molecules. 2016 Feb 4;21 (2) :185.