365462-23-3|Darexaban|N-(2-Hydroxy-6-(4-methoxybenzamido)phenyl)-4-(4-methyl-1,4-diazepan-1-yl)benzamide|-范德生物科技公司

Darexaban

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names：
N-(2-Hydroxy-6-(4-methoxybenzamido)phenyl)-4-(4-methyl-1,4-diazepan-1-yl)benzamide
CAS号：
365462-23-3
MDL Number：
MF(分子式)： C27H30N4O4 MW(分子量)： 474.561
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Darexaban
英文别名	YM150; YM 150; YM150; Darexaban, Tanexaban.
CAS号	365462-23-3
SMILES	O=C(NC1=C(NC(C2=CC=C(OC)C=C2)=O)C=CC=C1O)C3=CC=C(N4CCN(C)CCC4)C=C3
Inchi	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)
InchiKey	IJNIQYINMSGIPS-UHFFFAOYSA-N
分子式 Formula	C27H30N4O4
分子量 Molecular Weight	474.561
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Darexaban(CAS:365462-23-3):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	Darexaban, also known as Tanexaban and YM-150, is a direct inhibitor of factor Xa created by Astellas Pharma. Darexaban and darexaban glucuronide selectively and competitively inhibit FXa, suppressing prothrombin activity at the sites of blood clot (thrombus) formation. This leads to a decrease in blood clot formation in a dose dependent manner. Reducing blood clot formation will decrease blood flow blockages, thus possibly lowering the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[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):1405-13. doi: 10.1111/jth.13025. Epub 2015 Jul 15. PubMed PMID: 26052866.

[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):213-25. doi: 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):431-41. doi: 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/s13318-013-0141-1. Epub 2013 Jun 11. PubMed PMID: 23754514.

[5] Kaku S, Suzuki M, Saitoh M, Funatsu T, Uemura T, Suzuki K, Iwatsuki Y, Kawasaki T. 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. Epub 2013 Apr 13. PubMed PMID: 23591155.

6: Kadokura T, Taniuchi Y, Inoue H, Saito M, Iwahana M, Yamada S, Urae A, Nakamura M. Effect of food on the pharmacokinetics of darexaban, an oral direct factor Xa inhibitor, in healthy Japanese subjects. Int J Clin Pharmacol Ther. 2013 Mar;51(3):200-6. doi: 10.5414/CP201804. PubMed PMID: 23211396.7: Kaku S, Uemura T, Saitoh M, Suzuki K, Iwatsuki Y, Funatsu T, Kawasaki T. Antithrombotic and anticoagulant effects of direct factor Xa inhibitor darexaban in rat and rabbit models of venous thrombosis. Eur J Pharmacol. 2013 Jan 15;699(1-3):40-7. doi: 10.1016/j.ejphar.2012.11.026. Epub 2012 Nov 29. PubMed PMID: 23200896.8: Hashimoto T, Suzuki K, Kihara Y, Iwatsubo T, Miyashita A, Heeringa M, Onkels H, Groenendaal D, Verheggen F, van Marle S, Usui T. Absorption, metabolism and excretion of darexaban (YM150), a new direct factor Xa inhibitor in humans. Xenobiotica. 2013 Jun;43(6):534-47. doi: 10.3109/00498254.2012.738045. Epub 2012 Nov 20. PubMed PMID: 23167531.9: Fuji T, Nakamura M, Takeuchi M. Darexaban for the prevention of venous thromboembolism in Asian patients undergoing orthopedic surgery: results from 2 randomized, placebo-controlled, double-blind studies. Clin Appl Thromb Hemost. 2014 Mar;20(2):199-211. doi: 10.1177/1076029612457810. Epub 2012 Sep 4. PubMed PMID: 22952213.10: Sakon M, Nakamura M. Darexaban (YM150) prevents venous thromboembolism in Japanese patients undergoing major abdominal surgery: Phase III randomized, mechanical prophylaxis-controlled, open-label study. Thromb Res. 2012 Sep;130(3):e52-9. doi: 10.1016/j.thromres.2012.06.009. Epub 2012 Jul 2. PubMed PMID: 22762942.1

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