| 生物活性： |
靶点：Thrombin
通路：Metabolic Enzyme&Protease
背景说明：是一种凝血酶 (thrombin) 抑制剂。
生物活性：Bivalirudin TFA is a synthetic 20 residue peptide which reversibly inhibits thrombin. [1] Bivalirudin-facilitated binding of MPO to BAEC resulted also in functional changes in terms of increased NO consumption as well as enhanced MPO-mediated redox modifications [3].
In Vitro：IC50 Value: Target: thrombin in vitro: Eptifibatide(8 mg/mL)added together with a low(70 ng/mL)concentration of bivalirudin(a direct thrombin inhibitor)effectively(approximately 90%)reduced platelet aggregation induced by thrombin(0.2 U/mL)[1]. In thrombin generation assay(TGA)，bivalirudin had no effect on these parameters up to 10 μmol/l [2].
In Vivo：in vivo: The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats [4].
动物实验：Three animals in the 500-mg/kg/24 h group，and 7 animals in the 2000-mg/kg/24 h group in the toxicokinetic assessment phase of the study were found dead or euthanized in extremis(following blood sampling). Plasma concentrations of bivalirudin appeared to be linear and dose independent [5].
数据来源文献：[1]. Ciborowski M， Tomasiak M. The in vitro effect of eptifibatide， a glycoprotein IIb/IIIa antagonist， on various responses of porcine blood platelets. Acta Pol Pharm. 2009 May-Jun;66(3):235-42.
[2]. Xu Y， Wu W， Wang L， Differential profiles of thrombin inhibitors (heparin， hirudin， bivalirudin， and dabigatran) in the thrombin generation assay and thromboelastography in vitro. Blood Coagul Fibrinolysis. 2013 Apr;24(3):332-8.
[3]. Rudolph V， Rudolph TK， Schopfer FJ， Bivalirudin decreases NO bioavailability by vascular immobilization of myeloperoxidase. J Pharmacol Exp Ther. 2008 Nov;327(2):324-31.
[4]. Zhang R， Huang Y， Zhang M， Bivalirudin Utilization in Rats Undergoing Cardiopulmonary Bypass: Preventing the Increase of Antiheparin/Platelet Factor 4 Antibody in Perioperative Period. Clin Appl Thromb Hemost. 2012 Aug 21. [Epub ahead of print]
[5]. Gleason TG， Chengelis CP， Jackson CB， A 24-hour continuous infusion study of bivalirudin in the rat. Int J Toxicol. 2003 May-Jun;22(3):195-206.
|
| 其它标识： |
EC：EINECS 274-570-6
SMILES：CC[C@H](C)[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](CC(=O)N)NC(=O)CNC(=O)CNC(=O)CNC(=O)CNC(=O)[C@@H]4CCCN4C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]5CCCN5C(=O)[C@@H](CC6=CC=CC=C6)N
|
| 基本信息： |
CAS：128270-60-0
中文名称：比伐卢定三氟乙酸盐
英文名称：Bivalirudin TFA
别名：;比伐卢定;比瓦尔丁;比伐芦定;三氟醋酸比伐卢定，三氟醋酸比伐芦定;三氟醋酸比伐卢定;
分子式：C98H138N24O33·C2HF3O2
分子量：2294.3
规格：100mg ; 20mg ; 50mg
溶解性：Soluble in Water ≥10mg/mL
纯度：≥98%
外观(性状)：White to off-white Solid
储存条件：Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
|
| 靶点： |
Thrombin |
扫一扫关注我们
