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) [1]. In thrombin generation assay (TGA), bivalirudin had no effect on these parameters up to 10 μmol/l [2]. 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 vivo: The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats [4]. 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].
Clinical trial: Antithrombotic Effects of Ticagrelor Versus Clopidogrel . Phase 4
分子式
C98N24O33H138
分子量
2294.34
CAS号
1191386-55-6
中文名称
三氟醋酸比伐卢定
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light
Powder
-80°C
2 years
-20°C
1 year
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
H2O : 100 mg/mL (43.59 mM; Need ultrasonic)
DMSO : ≥ 31 mg/mL (13.51 mM)
*"≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.4359 mL
2.1793 mL
4.3586 mL
5 mM
0.0872 mL
0.4359 mL
0.8717 mL
10 mM
0.0436 mL
0.2179 mL
0.4359 mL
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: