Bivalirudin trifluoroacetate salt

Names

[ Name ]:
Bivalirudin trifluoroacetate salt

[Synonym ]:
Bivalirudin Trifluoroacetate
Angiox
L-Leucine, D-phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamy 
l-L-α-glutamyl-L-tyrosyl-
D-Phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamyl-L-α-glutamyl-L-tyrosyl-L-leucine
D-Phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamyl-L-α-g lutamyl-L-tyrosyl-L-leucine
L-leucine, D-phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamyl-L-α-glutamyl-L-tyrosyl-
bivalirudina
Hirulog-1
Bivalirudin
Hirulog
Angiomax
BG-8967
Bivalirudin (Trifluoroacetate)

Biological Activity

[Description]:

Bivalirudin Trifluoroacetate is a synthetic 20 residue peptide which reversibly inhibits thrombin.IC50 Value:Target: thrombinin 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

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Thrombin

[In Vivo]

Bivalirudin (2 mg/kg) delays both the time for appearance of first thrombus and the time for occlusion in P2Y12+/+ arteries, although neither prevented vessel occlusion[2].

[References]

[1]. Bates ER, et al. Bivalirudin: an anticoagulant option for percutaneous coronary intervention.Expert Rev Cardiovasc Ther. 2004 Mar;2(2):153-62.

[2]. André P, et al. Anticoagulants (thrombin inhibitors) and aspirin synergize with P2Y12 receptor antagonism in thrombosis.Circulation. 2003 Nov 25;108(21):2697-703.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₉₈H₁₃₈N₂₄O₃₃

[ Molecular Weight ]:
2295.31

[ PSA ]:
901.57000

[ LogP ]:
-2.24

[ Index of Refraction ]:
1.675

[ Storage condition ]:
?20°C

Safety Information

[ HS Code ]:
2942000000

Customs

[ HS Code ]: 2942000000