BIBR-1048
(Synonyms: 达比加群酯; BIBR 1048) 目录号 : GC15180
A prodrug form of dabigatran
Cas No.:211915-06-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dabigatran etexilate is a potent, selective and competitive inhibitor of thrombin. It is an oral prodrug of dabigatran. Ki=4.5 nM for human thrombin and IC50=10 nM for thrombin-induced platelet aggregation. [1] [2]
Thrombin is protein that proteolytically cleaved from coagulation factor II as the initial step in the coagulation cascade. It transforms fibrinogen into fibrin and activates other factors in function in blood homeostasis, wound healing and inflammation.
In vitro, dabigatran showed anticoagulant effects in a concentration-dependent manner. It doubled the activated partrial thromboplastin time, prothrombin time and ecarin clotting in human PPP. [1]
In rats and rhesus monkeys, activated partial throboplastin time was extended by dabigaran.
Rats orally administrated with dabigatran etexilate exerted anticoagulant effects in a dose and time –dependent manner. [1]
Compared with warfarin, dabigatran administered orally (150 mg dose) in patients with atrial fibraillation, exhibited lower rates of stroke and systemic embolism but similar rates of major hemorrhage. [2]
References:
1. Wienen W, Stassen JM, Priepke H 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.
2. Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrial
fibrillation. N Engl J Med. 2009 Sep 17;361(12):1139-51.
| Cas No. | 211915-06-9 | SDF | |
| 别名 | 达比加群酯; BIBR 1048 | ||
| 化学名 | ethyl 3-[[2-[[4-[(Z)-N'-hexoxycarbonylcarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate | ||
| Canonical SMILES | CCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N | ||
| 分子式 | C34H41N7O5 | 分子量 | 627.73 |
| 溶解度 | ≥ 30 mg/mL in DMSO, ≥ 22.13 mg/mL in EtOH | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.593 mL | 7.9652 mL | 15.9304 mL |
| 5 mM | 0.3186 mL | 1.593 mL | 3.1861 mL |
| 10 mM | 0.1593 mL | 0.7965 mL | 1.593 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。