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Edoxaban tosylate monohydrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Edoxaban tosylate monohydrate图片
CAS NO:1229194-11-9
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
Edoxaban (DU-176b) 一水合物是一种具有口服活性、高效、选择性和直接的因子 Xa (FXa) 抑制剂，对游离人 FXa 和凝血酶原酶的 Kis 分别为 0.561 和 2.98 nM。
Cas No.1229194-11-9
别名依度沙班对甲苯磺酸盐一水化合物,DU-176b monohydrate
化学名N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide;4-methylbenzenesulfonic acid;hydrate
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)O.CN1CCC2=C(C1)SC(=N2)C(=O)NC3CC(CCC3NC(=O)C(=O)NC4=NC=C(C=C4)Cl)C(=O)N(C)C.O
分子式C31H40ClN7O8S2
分子量738.27
溶解度≥ 36.9 mg/mL in DMSO, ≥ 5.78 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Factor Xa (FXa), a key serine protease, is a promising target enzyme for the prophylaxis and treatment of thromboembolic diseases. Edoxaban tosylate monohydrate is a novel antithrombotic agent that directly inhibits FXa activity.

In vitro: Edoxaban tosylate monohydrate (DU-176b) inhibited FXa with Ki values of 0.561 nM for free FXa, 2.98 nM for prothrombinase, and exhibited >10 000-fold selectivity for FXa. DU-176b doubled prothrombin time and activated partial thromboplastin time in human plasma. DU-176b did not impair platelet aggregation by ADP, collagen or U46619 [1].

In vivo: DU-176b dose-dependently inhibited thrombus formation in rat and rabbit thrombosis models, although bleeding time in rats was not significantly prolonged at an antithrombotic dose [1].

Clinical trial: A previous study determined the mass balance and pharmacokinetics of edoxaban in humans after oral administration of [14C]edoxaban. The mass balance of edoxaban study showed unchanged edoxaban as the most abundant component. Edoxaban was eliminated through multiple pathways, but each accounts for only a small amount of overall elimination [2].

References:
[1] Furugohri T, Isobe K, Honda Y, Kamisato-Matsumoto C, Sugiyama N, Nagahara T, Morishima Y, Shibano T.  DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008;6(9):1542-9.
[2] Bathala MS, Masumoto H, Oguma T, He L, Lowrie C, Mendell J.  Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans. Drug Metab Dispos. 2012;40(12):2250-5.