Bivalirudin
Cat. No.: DC29133
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Chemical Structure
128270-60-0
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Field of application
Bivalirudin, a peptide anticoagulant,direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
| Cas No.: |
128270-60-0 |
| Chemical Name: |
H-D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH |
| Synonyms: |
BG-8967; BG 8967; BG8967; Bivalirudin Trifluoroacetate; Brand name: Angiomax Angiox. |
| SMILES: |
O=C(N1[C@@H](CCC1)C(N[C@@H](CCCNC(N)=N)C(N2[C@@H](CCC2)C(NCC(NCC(NCC(NCC(N[C@@H](CC(N)=O)C(NCC(N[C@@H](CC(O)=O)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N4[C@@H](CCC4)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@ |
| Formula: |
C100H139F3N24O35 |
| M.Wt: |
2294.3402 |
| Purity: |
>99% |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
Bivalirudin Trifluoroacetate is a synthetic 20 residue peptide which reversibly inhibits thrombin. |
| Target: |
thrombin |
| 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 . 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].Phase 4 |
| 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]. |
| 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. |
MSDS
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| MSDS_13183_DC29133_128270-60-0 |
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