Dabigatran-d3
(Synonyms: BIBR 953-d3; BIBR 953ZW-d3) 目录号 : GC49682
An internal standard for the quantification of dabigatran
Cas No.:1246817-44-6
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
Dabigatran-d3 is intended for use as an internal standard for the quantification of dabigatran by GC- or LC-MS. Dabigatran is an inhibitor of thrombin (Ki = 0.0045 µM) and an active metabolite of the thrombin inhibitor prodrug dabigatran etexilate .1,2 It also inhibits trypsin (Ki = 0.0503 µM) but is selective for thrombin and trypsin over plasmin, Factor Xa, activated protein C, and tissue plasminogen activator (tPA; Kis = 1.695, 3.76, 20.93, and 45.36 µM, respectively).1
1.Hauel, N.H., Nar, H., Priepke, H., et al.Structure-based design of novel potent nonpeptide thrombin inhibitorsJ. Med. Chem.45(9)1757-1766(2002) 2.Eisert, W.G., Hauel, N., Stangier, J., et al.Dabigatran: An oral novel potent reversible nonpeptide inhibitor of thrombinArterioscler. Thromb. Vasc. Biol.30(10)1885-1889(2010)
| Cas No. | 1246817-44-6 | SDF | Download SDF |
| 别名 | BIBR 953-d3; BIBR 953ZW-d3 | ||
| Canonical SMILES | OC(CCN(C1=CC=CC=N1)C(C2=CC=C(C(N=C3CNC4=CC=C(C=C4)C(N)=N)=C2)N3C([2H])([2H])[2H])=O)=O | ||
| 分子式 | C25H22D3N7O3 | 分子量 | 474.5 |
| 溶解度 | DMSO: slightly soluble | 储存条件 | -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 | 2.1075 mL | 10.5374 mL | 21.0748 mL |
| 5 mM | 0.4215 mL | 2.1075 mL | 4.215 mL |
| 10 mM | 0.2107 mL | 1.0537 mL | 2.1075 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。
Comparison of calibrated dilute thrombin time and aPTT tests with LC-MS/MS for the therapeutic monitoring of patients treated with dabigatran etexilate
Thromb Haemost 2013 Sep;110(3):543-9.PMID:23783171DOI:10.1160/TH13-03-0202
Ways to monitor dabigatran etexilate (DE) therapy would be useful in certain situations. Functional assays such as aPTT or Hemoclot® Thrombin Inhibitor (HTI) have been proposed to evaluate dabigatran concentrations, but previous findings are based on in vitro studies and results must be confirmed in clinical samples. The aim of this study was to compare aPTT and HTI measurements with liquid chromatography-tandem mass spectrometry (LC-MS/MS) measurements of dabigatran in plasma samples from DE treated patients. Seventy-one plasma samples were included. aPTT was performed using STA-CKPrest® and SynthASil®. HTI was performed according to instructions from the manufacturer. The LC-MS/MS method utilised Dabigatran-d3 as internal standard. The plasma concentration range was 0 to 645 ng/ml as measured by LC-MS/MS. Overall, the HTI and LC-MS/MS analyses correlated well (r²=0.97). The Bland-Altman analysis showed a mean difference of 9 ng/ml (SD: 20 ng/ml). However, the HTI performed poorly at concentrations <50 ng/ml. LC-MS/MS was sensitive (limit of quantification 1.1 ng/ml) and specific for dabigatran. The aPTT methods did not correlate well with plasma concentrations measured by LC-MS/MS (r² = 0.59 with SynthASil® and 0.50 with STA-CKPrest®). In conclusion, the poor sensitivity, the important inter-individual variability, and the poor correlation with LC-MS/MS preclude the use of aPTT to estimate dabigatran concentrations. Due to its small inter-individual variability and good agreement with LC-MS/MS measurements, we recommend the use of HTI assays to rather accurately estimate concentrations of dabigatran >50 ng/ml. Quantification of lower dabigatran levels in DE-treated patients requires the "reference" LC-MS/MS method.