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Darexaban glucuronide

货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
FMK14098-100mg 100mg >98% ¥ 0.00 ¥ 0.00 Get quote
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中文别名 Darexaban glucuronide
英文别名 YM-222714; YM 222714; YM222714; Darexaban glucuronide
CAS号 432029-12-4
SMILES O[C@H]([C@H]([C@@H]([C@@H](C(O)=O)O1)O)O)[C@@H]1OC2=CC=CC(NC(C3=CC=C(OC)C=C3)=O)=C2NC(C4=CC=C(N5CCN(C)CCC5)C=C4)=O
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 Molecular Weight C33H38N4O10
分子量 Formula 650.685
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 Soluble in DMSO
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 glucuronide(CAS:432029-12-4):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。
IntroductionDarexaban 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.
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[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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