| 中文名称 |
Bivalirudin TFA
|
| 中文别名 |
三氟醋酸比伐卢定
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| 英文名称 |
Bivalirudin TFA
|
| 英文别名 |
Bivalirudin TFA
|
| Cas No. |
1191386-55-6
|
| 分子式 |
C98H138N24O33
|
| 分子量 |
2180.29
|
| 包装储存 |
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
|
| 详情描述 |
Bivalirudin TFA 是20个氨基多肽,可逆地抑制凝血酶。
|
| 产品详情 |
Bivalirudin TFA 是20个氨基多肽,可逆地抑制凝血酶。
|
| 生物活性 |
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
|
| 性状 |
Solid
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Sealed storage, away from moisture and lightPowder -80°C 2 years;-20°C 1 year
|
| ClinicalTrial |
|
| SequenceShortening |
{d-Phe}-PRPGGGGNGDFEEIPEEYL
|
| Sequence |
{d-Phe}-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu
|
| 参考文献 |
[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.
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| 溶解度数据 |
In Vitro: H2O : ≥ 50 mg/mL (21.79 mM)DMSO : ≥ 31 mg/mL (13.51 mM)
|
[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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。