比伐卢定 T5519

Product Introduction
Bioactivity


英文名: Bivalirudin

描述: Bivalirudin (BG-8967) 是一种直接凝血酶(thrombin)抑制剂，是一种肽类抗凝剂，可在侵入性心脏病，特别是在经皮冠状动脉介入中用于抗凝。

动物实验: Animals were randomly assigned to one of five groups: control (no aspirin or hirulog); aspirin alone (10 mg/kg); aspirin plus low-dose hirulog (0.2 mg/kg bolus followed by 0.5 mg/kg/hr); aspirin plus medium-dose hirulog (0.4 mg/kg bolus followed by 1.0 mg/kg/hr); or aspirin plus high-dose hirulog (0.6 mg/kg bolus followed by 1.5 mg/kg/hr). Hirulog was infused before surgery and continued until termination of the experiment 30 minutes after endarterectomy [3].

体外活性: Whereas 0.1 microM-hirudin and 0.1 microM-Bivalirudin (i.e. less than 10% of the concentration of prothrombin in plasma) inhibited Factor X, Factor V, and prothrombin activation. Concentrations of hirudin and hirulog-1 equimolar to and 5 times greater than those of alpha-thrombin respectively abrogated Factor V activation by exogenous alpha-thrombin [2].

体内活性: Deposition in aspirin-treated groups receiving low-, medium-, and high-dose Bivalirudin decreased in a dose-dependent manner by 37%, 44%, and 56%, respectively. As the dose of Bivalirudin was increased, the plasma Bivalirudin levels and activated partial thromboplastin time ratios (final: initial) also increased in a dose-dependent manner. The mean plasma Bivalirudin levels ranged from 0.74 micrograms/ml in the low-dose Bivalirudin group to 2.55 micrograms/ml in the high-dose Bivalirudin group, and the corresponding activated partial thromboplastin time ratios were 1.5 and 3.3 [3].

存储条件: keep away from moisturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mM


关键字: BG8967 | anticoagulation | invasive | peptide | coronary | Inhibitor | platelets | percutaneous | Bivalirudin | anticoagulant | Thrombin | inhibit | cardiology | BG 8967

相关产品: Enoxaparin sodium | Edoxaban | Melagatran | Avatrombopag | Efegatran sulfate | AEBSF hydrochloride | Dabigatran etexilate | Dabigatran ethyl ester hydrochloride | Dabigatran ethyl ester | p-Hydroxycinnamic acid

相关库: ReFRAME Related Library | Peptide Compound Library | Protease Inhibitor Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途