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非天然氨基酸及其它砌块合成
三氟醋酸比伐卢定
名称
三氟醋酸比伐卢定
分子结构式
CAS号
1191386-55-6
分子式
C98H138N24O33.C2HF3O2
分子量
2294.34
作用靶点
Thrombin
序列号
{D-Phe}-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu
短序列号
{D-Phe}-PRPGGGGNGDFEEIPEEYL
国际标识符代码
OIRCOABEOLEUMC-ONGBENNUSA-N
溶解度
≥ 31 mg/mL
水中溶解度
≥ 50 mg/mL
纯度
≥98%
引用文献
[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.
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Bivalirudin TFA is a synthetic 20 residue peptide which reversibly inhibits thrombin. 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) . In thrombin generation assay (TGA), bivalirudin had no effect on these parameters up to 10 μmol/l . 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. The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats. 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. Clinical trial: Antithrombotic Effects of Ticagrelor Versus Clopidogrel.