N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide

Product Name: N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide
CAS No.: 365462-23-3
Chemical Name: N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide
Synonyms: YM-150;YM 150);Tanexaban;Darexaban (YM150;Darexaban, Tanexaban;Darexaban, 10 mM in DMSO;N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide;N-(3-Hydroxy-2-(4-(4-methyl-1,4-diazepan-1-yl)benzamido)phenyl)-4-methoxybenzamide;N-[2-hydroxy-6-[(4-methoxybenzoyl)amino]phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide;Benzamide, N-[2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)benzoyl]amino]-3-hydroxyphenyl]-4-methoxy-
CBNumber: CB92484869
Molecular Formula: C27H30N4O4
Formula Weight: 474.56
MOL File: 365462-23-3.mol

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N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide Property

Boiling point:: 557.2±50.0 °C(Predicted)
Density: 1.280±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 250 mg/mL (526.81 mM; Need ultrasonic)
pka: 9.11±0.40(Predicted)
form: Solid
color: Off-white to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Biosynth Carbosynth

Product number: FD36340
Product name: Darexaban
Packaging: 5mg
Price: $550
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD36340
Product name: Darexaban
Packaging: 10mg
Price: $990
Updated: 2021/12/16

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N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide Chemical Properties,Usage,Production

Uses

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 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].

References

[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. DOI:10.1021/jm200868m
[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. DOI:10.1016/j.thromres.2013.03.016
[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. DOI:10.3390/molecules21020185

N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide Suppliers

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365462-23-3, N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamideRelated Search:

Darexaban (YM150

YM 150)

YM-150

N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide

Tanexaban

N-[2-hydroxy-6-[(4-methoxybenzoyl)amino]phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide

N-(3-Hydroxy-2-(4-(4-methyl-1,4-diazepan-1-yl)benzamido)phenyl)-4-methoxybenzamide

Darexaban, Tanexaban

Factor Xa,Serine endopeptidases,time,Darexaban,YM-150,Ser/Thr Protease,Fxa,oral,antithrombotic,Inhibitor,prothrombin,Serine proteases,Threonine proteases,anticoagulant,inhibit

Benzamide, N-[2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)benzoyl]amino]-3-hydroxyphenyl]-4-methoxy-

Darexaban, 10 mM in DMSO

365462-23-3