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Bivalirudin Trifluoroacetate

现货
Catalog No.
A3244
凝血酶抑制剂
组合的产品项目
规格价格库存 数量
100mg
¥ 1,250.00
Ship with 10-14 days
500mg
¥ 3,780.00
Ship with 10-14 days

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt2180.29
Cas No.128270-60-0
FormulaC98H138N24O33
SynonymsBivalirudin
Solubility≥54.5 mg/mL in DMSO with gentle warming, ≥42 mg/mL in EtOH with gentle warming, ≥86.2 mg/mL in H2O with gentle warming
Chemical Name(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
SDFDownload SDF
Canonical SMILESCC[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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

体外实验 [1]:

样品

血小板缺乏的血浆

制备方法

上述化合物可溶解于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

1.5 ~ 30 μg/mL

实验结果

在血小板缺乏的血浆中,Bivalirudin呈剂量依赖性地延迟凝血酶形成,上述作用不受激活剂影响。 肌动蛋白激活后,凝血酶峰值水平逐渐降低(从1.5 μg/mL的21.5% ± 9.2%到30 μg/mL的69.9% ± 12.3%)。以组织因子为触发因素,凝血酶峰值水平下降幅度相对缓慢。在30 μg/mL剂量下,凝血酶峰值水平仅降低了29.4% ± 6.2%。

动物实验 [2]:

动物模型

凝血激酶诱导的血栓形成小鼠模型

给药剂量

1 μmol/kg;静脉注射

实验结果

在凝血激酶诱导的血栓形成小鼠模型中,Bivalirudin胶束在肺血栓中积累,比游离Bivalirudin高10倍。此外,Bivalirudin胶束显著延长半衰期,从而增加Bivalirudin的生物利用度。在肺血栓形成模型和氯化铁诱导的颈动脉血栓形成模型中,Bivalirudin胶束均比游离Bivalirudin具有显著较高的抗凝血活性。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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.

质量控制

化学结构

Bivalirudin Trifluoroacetate