Darexaban

• 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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 3

• CAS Number:

  [365462-23-3]