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Darexaban glucuronide

NMR下載 COA and HPLC MSDS下載
names：
(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(3-(4-methoxybenzamido)-2-(4-(4-methyl-1,4-diazepan-1-yl)benzamido)phenoxy)tetrahydro-2H-pyran-2-carboxylic acid
CAS號：
432029-12-4
MDL Number：
MF(分子式)： C33H38N4O10 MW(分子量)： 650.685
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	Darexaban glucuronide
英文別名	YM-222714; YM 222714; YM222714; Darexaban glucuronide
CAS號	432029-12-4
Inchi	InChI=1S/C33H38N4O10/c1-36-15-4-16-37(18-17-36)21-11-7-19(8-12-21)31(42)35-25-23(34-30(41)20-9-13-22(45-2)14-10-20)5-3-6-24(25)46-33-28(40)26(38)27(39)29(47-33)32(43)44/h3,5-14,26-29,33,38-40H,4,15-18H2,1-2H3,(H,34,41)(H,35,42)(H,43,44)/t26-,27-,28+,29-,33+/m0/s1
InchiKey	IOUMBCGOXOKZAE-CLIYFGAVSA-N
分子式 Formula	C33H38N4O10
分子量 Molecular Weight	650.685
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產品說明	Darexaban glucuronide(CAS:432029-12-4):僅限應用于工業或者科學研究過程中非醫療目的，不應用于人類或動物的臨床診斷以及治過程療，該產品非藥用，非食用。
Introduction	Darexaban glucuronide, also known as YM-222714, is the major component in plasma after oral administration of darexaban to humans and is the pharmacologically active metabolite. Darexaban (YM150) is a direct inhibitor of factor Xa. It is an experimental drug that acts as an anticoagulant and antithrombotic to prevent venous thromboembolism after a major orthopaedic surgery, stroke in patients with atrial fibrillation and possibly ischemic events in acute coronary syndrome. It is used in form of the maleate. The development of darexaban was discontinued in September 2011.
Application1
Application2
Application3

警示圖
危險性	Warning
危險性警示
安全聲明
安全防護
備注

[1]Ishihara T, Koga Y, Mori K, Sugasawa K, Iwatsuki Y, Hirayama F. Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates. Bioorg Med Chem. 2014 Nov 15;22(22):6324-32. doi: 10.1016/j.bmc.2014.09.059. Epub 2014 Oct 19. PubMed PMID: 25438755.

[2]Groenendaal D, Strabach G, Garcia-Hernandez A, Kadokura T, Heeringa M, Mol R, Eltink C, Onkels H. The pharmacokinetics of darexaban (YM150), an oral direct factor Xa inhibitor, are not affected by ketoconazole, a strong inhibitor of CYP3A and P-glycoprotein. Clin Pharmacol Drug Dev. 2014 May;3(3):194-201. doi: 10.1002/cpdd.93. Epub 2014 Mar 3. PubMed PMID: 27128609.

[3] Kadokura T, Oikawa K, Miyata K, Murase T, Nakamura M. Clinical Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Darexaban, an Oral Direct Factor Xa Inhibitor, in Healthy Elderly Japanese Subjects. Clin Pharmacol Drug Dev. 2013 Oct;2(4):328-35. doi: 10.1002/cpdd.50. Epub 2013 Aug 16. PubMed PMID: 27121937.

[4] 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.

[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: Groenendaal D, Strabach G, Garcia-Hernandez A, Kadokura T, Heeringa M, Mol R, Eltink C, Onkels H. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4. Br J Clin Pharmacol. 2013 Feb;75(2):440-9. doi: 10.1111/j.1365-2125.2012.04346.x. PubMed PMID: 22642721; PubMed Central PMCID: PMC3579259.10: Shiraga T, Yajima K, Teragaki T, Suzuki K, Hashimoto T, Iwatsubo T, Miyashita A, Usui T. 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. Biol Pharm Bull. 2012;35(3):413-21. PubMed PMID: 22382330.1

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