Edoxaban tosylate
(Synonyms: 依度沙班对甲苯磺酸盐; DU-176b) 目录号 : GC35962
A potent inhibitor of Factor Xa
Cas No.:480449-71-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Kis = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively).1 It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
1.Furugohri, T., Isobe, K., Honda, Y., et al.DU-176b, a potent and orally active factor Xa inhibitor: In vitro and in vivo pharmacological profilesJ. Thromb. Haemost.6(9)1542-1549(2008)
| Cas No. | 480449-71-6 | SDF | |
| 别名 | 依度沙班对甲苯磺酸盐; DU-176b | ||
| Canonical SMILES | O=C(N(C)C)[C@@H](CC1)C[C@H]([C@H]1NC(C(NC(C=C2)=NC=C2Cl)=O)=O)NC(C3=NC(CC4)=C(CN4C)S3)=O.O=S(C5=CC=C(C)C=C5)(O)=O | ||
| 分子式 | C31H38ClN7O7S2 | 分子量 | 720.26 |
| 溶解度 | DMSO : 50 mg/mL (69.42 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3884 mL | 6.9419 mL | 13.8839 mL |
| 5 mM | 0.2777 mL | 1.3884 mL | 2.7768 mL |
| 10 mM | 0.1388 mL | 0.6942 mL | 1.3884 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Edoxaban tosylate
Am J Cardiovasc Drugs 2011;11(2):129-35.PMID:21446778DOI:10.2165/11533660-000000000-00000.
Daiichi Sankyo is developing Edoxaban tosylate (DU 176b; DU-176; DU-176b; DU176b) as an orally active direct factor Xa inhibitor for the prevention of stroke and the prevention and treatment of venous thromboembolism. Two dosing regimens of Edoxaban tosylate are being compared with warfarin over 24 months in the ENGAGE AF TIMI 48 trial (NCT00781391) in over 21 000 patients with atrial fibrillation in North and South America, Africa, Asia, Europe, Australia, and New Zealand. Edoxaban tosylate is also being compared with warfarin in the treatment and prevention of recurrent thromboembolic events in approximately 7500 patients with deep-vein thrombosis and/or pulmonary embolism in the HOKUSAI VTE trial (NCT00986154) being conducted in 40 countries. This review discusses the development history and scientific profile of this new compound.