GlpBio

Bivalirudin Trifluoroacetate

目录号: GC10448纯度: >98%同义词: 比伐卢定,Bivalirudin
COASDSData Sheet
A thrombin inhibitor
Bivalirudin Trifluoroacetate
Cas No.: 128270-60-0
规格价格库存数量操作
100mg¥893.00现货
1
500mg¥2,940.00现货
1
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

In vitro experiment [1]:

Samples

Platelet-poor plasma

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.

Reacting condition

1.5 ~ 30 μg/mL

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]:

Animal models

A thromboplastin-induced thrombosis mouse model

Dosage form

1 μmol/kg; i.v.

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.

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.

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.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
128270-60-0
同义词
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
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 g/mol
溶解性
≥ 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
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol