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首页 / 抑制剂/激动剂 / 代谢酶 / 凝血酶 / Dabigatran etexilate

达比加群酯 /Dabigatran etexilate {[allProObj[0].p_purity_real_show]}

货号：A249359 同义名： BIBR 1048

Dabigatran etexilate是Dabigatran的活性前体药物，对凝血酶的选择性抑制作用Ki为4.5 nM。

Dabigatran etexilate 化学结构 CAS号：211915-06-9
Dabigatran etexilate 化学结构
CAS号：211915-06-9
Dabigatran etexilate 3D分子结构
CAS号：211915-06-9
Dabigatran etexilate 化学结构 CAS号：211915-06-9
Dabigatran etexilate 3D分子结构 CAS号：211915-06-9
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Dabigatran etexilate 纯度/质量文件 产品仅供科研

货号：A249359 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Thrombin ↓ 其他靶点 纯度
Dabigatran +++

Thrombin, IC50: 9.3 nM

 		98%
Dabigatran etexilate ✔ 98%
Argatroban 99%+
Heparin sodium salt ✔ ≥150 u/mg
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dabigatran etexilate 生物活性

靶点

  • Thrombin
描述 Thrombin is produced by the proteolytic cleavage of prothrombin and serves as a multifunctional serine protease with a central role in blood coagulation, platelet activation and wound healing. In pathological conditions, thrombus formation eventually leads to vascular occlusion which, inturn, can result in the development of thromboembolic disease. Dabigatran etexilate is an orally active prodrug of dabigatran which is a reversible and selective, direct thrombin inhibitor undergoing advanced clinical development. Dabigatran selectively and reversibly inhibited human thrombin (Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 10 nM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP (platelet-poor plasma) at concentrations of 0.23, 0.83 and 0.18 μM, respectively. In vivo, dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively[3]. In a modified Wessler model, bolus administration of dabigatran (0.01 - 0.1 mg/kg) reduced thrombus formation dose-dependently, with an ED50 of 0.033 mg/kg and complete inhibition at 0.1 mg/kg[4].

Dabigatran etexilate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02170922 Healthy Phase 1 Completed - -
NCT02666157 Atrial Fibrillation Phase 4 Unknown December 2018 Taiwan ... 展开 >> National Cheng Kung University Hospital Recruiting Tainan, Tainan City, Taiwan, 704 Contact: Ting-Hsing Chao, MD    886-6-2353535 ext 2382    chaoth@mail.ncku.edu.tw    Principal Investigator: Ting-Hsing Chao, MD          Sub-Investigator: Ju-Yi Chen, MD and PhD          Sub-Investigator: Cheng-Han Lee, MD and PhD          Sub-Investigator: Chih-Chan Lin, MD          Sub-Investigator: Chih-Hung Chen, MD          Sub-Investigator: Liang-Miin Tsai, MD          Sub-Investigator: Li-Jen Lin, MD          Sub-Investigator: Wei-Chuan Tsai, MD          Sub-Investigator: Ping-Yen Liu, MD and PhD          Tainan Hospital Ministry of Health and Welfare Not yet recruiting Tainan, Tainan City, Taiwan, 704 Contact: Li-Dan Yang, MD    886-6-2200055 ext 9    litannyang@yahoo.com.tw    Principal Investigator: Li-Dan Yang, MD          National Cheng Kung University Hospital Dou-Liou Branch Not yet recruiting Dou-Liou City, Taiwan, 640 Contact: Yang-Cheh Hsueh, MD    886-5-5332121 ext 5101    p308378@dou6.hosp.ncku.edu.tw    Principal Investigator: Yang-Cheh Hsueh, MD          Sub-Investigator: Yuen-Ting Sung, MD and PhD          E-DA Hospital Not yet recruiting Kaohsiung, Taiwan, 824 Contact: Wei-Kung Tseng, MD and PhD    886-7-6150011 ext 5005    arthurtseng@me.com    Principal Investigator: Wei-Kung Tseng, MD and PhD          Tainan Municipal Hospital Recruiting Tainan, Taiwan, 701 Contact: I-Chih Chen, MD    886-6-2609926 ext 212045    ichih1230@yahoo.com.tw    Principal Investigator: I-Chih Chen, MD          Sub-Investigator: Ruei-Chang Zeng, MD 收起 <<
NCT01468155 Atrial Fibrillation Phase 4 Completed - Canada, Ontario ... 展开 >> London Health Sciences Center London, Ontario, Canada, N6A 5A5 收起 <<

Dabigatran etexilate 参考文献

[1]McKellar SH, Abel S, et al. Effectiveness of dabigatran etexilate for thromboprophylaxis of mechanical heart valves. J Thorac Cardiovasc Surg. 2011 Jun;141(6):1410-6.

[2]Wienen W, Stassen JM, et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.

[3]Wienen W, Stassen JM, Priepke H, Ries UJ, Hauel N. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007;98(1):155-162.

[4]Wienen W, Stassen JM, Priepke H, Ries UJ, Hauel N. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007;98(2):333-338.

Dabigatran etexilate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.97mL

1.59mL

0.80mL

15.93mL

3.19mL

1.59mL

Dabigatran etexilate 技术信息

CAS号211915-06-9
分子式C34H41N7O5
分子量 627.733
别名 BIBR 1048
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(167.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

Tags: Dabigatran etexilate | BIBR 1048 | Thrombin | AmBeed-信号通路专用抑制剂 | Dabigatran etexilate 纯度/质量文件 | Dabigatran etexilate 亚型比较 | Dabigatran etexilate 生物活性 | Dabigatran etexilate 临床数据 | Dabigatran etexilate 参考文献 | Dabigatran etexilate 实验方案 | Dabigatran etexilate 技术信息

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