Bivalirudin Trifluoroacetate
(Synonyms: 比伐卢定,Bivalirudin) 目录号 : GC10448
A thrombin inhibitor
Cas No.:128270-60-0
Sample solution is provided at 25 µL, 10mM.
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BivalirudinTrifluoroacetate is a specific, reversible and direct thrombin inhibitor with a predictable anticoagulant effect.
In patients with normal or mildly impaired renal function, bivalirudin exihibited several notable mechanistic advantages when compared with unfractionated heparin. Bivalirudin showed activity against clot-bound thrombin, inhibition of thrombin-induced platelet activation, short plasma half-life (25 minutes)[1]. Bivalirudin inhibited both circulating thrombin and fibrin bound thrombin directly by binding to thrombin catalytic site and anion-binding exosite I in a concentration-dependent manner. Bivalirudin prolonged activated partial thromboplastin time, prothrombin time, thrombin time and activated clotting time (ACT). ACT levels activated by bivalirudin showed no correlation with its clinical efficacy [1]. When compared to heparin alone or heparin in combination with-a GpIIb/IIIa inhibitor, bivalirudin had shown less in-hospital major bleeding. Bivalirudin was safe and effective during percutaneous coronary intervention (PCI) in patients with heparin-induced thrombocytopenia, indicated the safety and efficacy of bivalirudin [1].
Reference:
[1]. Shammas N W. Bivalirudin: pharmacology and clinical applications[J]. Cardiovascular drug reviews, 2005, 23(4): 345-360.
| In vitro experiment [1]: | |
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Samples |
Platelet-poor plasma |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
1.5 ~ 30 μg/mL |
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Applications |
In platelet-poor plasma, Bivalirudin dose-dependently delayed thrombin formation regardless of the activators. Under actin activation, thrombin peak levels decreased progressively (21.5% ± 9.2% at 1.5 μg/mL to 69.9% ± 12.3% at 30 μg/mL). With tissue factor as a trigger, the decrease was more gradual. The peak level of thrombin was only reduced by 29.4% ± 6.2% at 30 μg/mL. |
| Animal experiment [2]: | |
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Animal models |
A thromboplastin-induced thrombosis mouse model |
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Dosage form |
1 μmol/kg; i.v. |
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Applications |
In a thromboplastin-induced lung thrombosis mouse model, Bivalirudin micelles were accumulated in lung thrombi 10-fold more than free Bivalirudin. Moreover, Bivalirudin micelles significantly prolonged the half-life time, increasing the bioavailability of Bivalirudin. In addition, Bivalirudin micelles showed significantly higher anticoagulant activity than free Bivalirudin in both the lung thrombosis model and the ferric chloride-induced carotid artery thrombosis model. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Tanaka KA, Szlam F, Sun HY, Taketomi T, Levy JH. Thrombin generation assay and viscoelastic coagulation monitors demonstrate differences in the mode of thrombin inhibition between unfractionated heparin and bivalirudin. Anesth Analg. 2007 Oct;105(4):933-9. [2]. She ZG, Liu X, Kotamraju VR, Ruoslahti E. Clot-targeted micellar formulation improves anticoagulation efficacy of bivalirudin. ACS Nano. 2014 Oct 28;8(10):10139-49. | |
| Cas No. | 128270-60-0 | SDF | |
| 别名 | 比伐卢定,Bivalirudin | ||
| 化学名 | (1Z,4Z,7Z,10Z,13Z,15S,16Z,19Z,21S,22Z,24S,25Z,27S,28Z,30S)-1-((S)-1-((S)-2-((Z)-(((S)-1-((R)-2-amino-3-phenylpropanoyl)pyrrolidin-2-yl)(hydroxy)methylene)amino)-5-guanidinopentanoyl)pyrrolidin-2-yl)-24-benzyl-30-((Z)-(((2S,3S)-1-((S)-2-((1Z,3S,4Z,6S,7Z,9S | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/C/N=C(O)/C/N=C(O)/C/N=C(O)/C/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@]2([H])CCCN2C([C@@](N)([H])CC3=CC=CC=C3)=O)([H])CCCNC(N)=N)=O)([H])CC(O)=N)([H])CC(O)=O)([H | ||
| 分子式 | C98H138N24O33 | 分子量 | 2180.29 |
| 溶解度 | ≥ 54.5 mg/mL in DMSO with gentle warming, ≥ 42 mg/mL in EtOH with gentle warming, ≥ 86.2 mg/mL in Water with gentle warming | 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 | 0.4587 mL | 2.2933 mL | 4.5865 mL |
| 5 mM | 0.0917 mL | 0.4587 mL | 0.9173 mL |
| 10 mM | 0.0459 mL | 0.2293 mL | 0.4587 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet