Darexaban (BioDeep_00000177962)

   

human metabolite blood metabolite


代谢物信息卡片


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

化学式: C27H30N4O4 (474.226694)
中文名称: N-[2-羟基-6-(4-甲氧基苯甲酰氨基)苯基]-4-(4-甲基-1,4-二氮杂庚烷-1-基)苯甲酰胺
谱图信息: 最多检出来源 Homo sapiens(blood) 95.24%

分子结构信息

SMILES: CN1CCCN(CC1)C2=CC=C(C=C2)C(=O)NC3=C(C=CC=C3O)NC(=O)C4=CC=C(C=C4)OC
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)

描述信息

D004791 - Enzyme Inhibitors > D011480 - Protease Inhibitors > D015842 - Serine Proteinase Inhibitors
D006401 - Hematologic Agents > D000925 - Anticoagulants > D000991 - Antithrombins
C78275 - Agent Affecting Blood or Body Fluid > C29750 - Thrombolytic Agent

同义名列表

4 个代谢物同义名

N-(2-Hydroxy-6-(4-methoxybenzamido)phenyl)-4-(4-methyl-1,4-diazepan-1-yl)benzamide; N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl)benzamide; YM150 CPD; Darexaban



数据库引用编号

7 个数据库交叉引用编号

分类词条

相关代谢途径

Reactome(0)

BioCyc(0)

PlantCyc(0)

代谢反应

0 个相关的代谢反应过程信息。

Reactome(0)

BioCyc(0)

WikiPathways(0)

Plant Reactome(0)

INOH(0)

PlantCyc(0)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

1 个相关的物种来源信息

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

  • PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。



文献列表

  • G Y H Lip, J L Halperin, P Petersen, G M Rodgers, D Pall, R W Renfurm. 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). Journal of thrombosis and haemostasis : JTH. 2015 Aug; 13(8):1405-13. doi: 10.1111/jth.13025. [PMID: 26052866]
  • Takeshi Kadokura, Makoto Kashiwa, Dorien Groenendaal, Marten Heeringa, Roelof Mol, Frank Verheggen, Alberto Garcia-Hernandez, Hartmut Onkels. Clinical pharmacokinetics, pharmacodynamics, safety and tolerability of darexaban, an oral direct factor Xa inhibitor, in healthy Caucasian and Japanese subjects. Biopharmaceutics & drug disposition. 2013 Nov; 34(8):431-41. doi: 10.1002/bdd.1858. [PMID: 23929659]
  • Tadashi Hashimoto, Katsuhiro Suzuki, Yukie Kihara, Takafumi Iwatsubo, Aiji Miyashita, Marten Heeringa, Hartmut Onkels, Dorien Groenendaal, Frank Verheggen, Sjoerd van Marle, Takashi Usui. Absorption, metabolism and excretion of darexaban (YM150), a new direct factor Xa inhibitor in humans. Xenobiotica; the fate of foreign compounds in biological systems. 2013 Jun; 43(6):534-47. doi: 10.3109/00498254.2012.738045. [PMID: 23167531]
  • Seiji Kaku, Mami Suzuki, Minori Saitoh, Toshiyuki Funatsu, Toshio Uemura, Ken-ichi Suzuki, Yoshiyuki Iwatsuki, Tomihisa Kawasaki. 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. Thrombosis research. 2013 May; 131(5):450-6. doi: 10.1016/j.thromres.2013.03.016. [PMID: 23591155]
  • Dorien Groenendaal, Gregory Strabach, Alberto Garcia-Hernandez, Takeshi Kadokura, Marten Heeringa, Roelof Mol, Charlotte Eltink, Hartmut Onkels. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4. British journal of clinical pharmacology. 2013 Feb; 75(2):440-9. doi: 10.1111/j.1365-2125.2012.04346.x. [PMID: 22642721]
  • Toshiyuki Funatsu, Atsushi Yamashita, Seiji Kaku, Yoshiyuki Iwatsuki, Yujiro Asada. Plasma factor Xa inhibition can predict antithrombotic effects of oral direct factor Xa inhibitors in rabbit atherothrombosis models. Thrombosis and haemostasis. 2012 Nov; 108(5):896-902. doi: 10.1160/th12-04-0267. [PMID: 23052641]
  • Toshifumi Shiraga, Kanako Yajima, Kenta Suzuki, Katsuhiro Suzuki, Tadashi Hashimoto, Takafumi Iwatsubo, Aiji Miyashita, Takashi Usui. Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine. Drug metabolism and disposition: the biological fate of chemicals. 2012 Feb; 40(2):276-82. doi: 10.1124/dmd.111.042614. [PMID: 22031623]
  • Toshifumi Shiraga, Kanako Yajima, Takuya Teragaki, Katsuhiro Suzuki, Tadashi Hashimoto, Takafumi Iwatsubo, Aiji Miyashita, Takashi Usui. Identification of enzymes responsible for the N-oxidation of darexaban glucuronide, the pharmacologically active metabolite of darexaban, and the glucuronidation of darexaban N-oxides in human liver microsomes. Biological & pharmaceutical bulletin. 2012; 35(3):413-21. doi: 10.1248/bpb.35.413. [PMID: 22382330]
  • Yoshiyuki Iwatsuki, Takayuki Sato, Yumiko Moritani, Takeshi Shigenaga, Mami Suzuki, Tomihisa Kawasaki, Toshiyuki Funatsu, Seiji Kaku. Biochemical and pharmacological profile of darexaban, an oral direct factor Xa inhibitor. European journal of pharmacology. 2011 Dec; 673(1-3):49-55. doi: 10.1016/j.ejphar.2011.10.009. [PMID: 22040919]
  • Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Shunichiro Hachiya, Keizo Sugasawa, Yuji Koga, Norio Seki, Ryouta Shiraki, Takeshi Shigenaga, Yoshiyuki Iwatsuki, Yumiko Moritani, Kenichi Mori, Takeshi Kadokura, Tomihisa Kawasaki, Yuzo Matsumoto, Shuichi Sakamoto, Shin-ichi Tsukamoto. 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. Journal of medicinal chemistry. 2011 Dec; 54(23):8051-65. doi: 10.1021/jm200868m. [PMID: 21995444]