Bivalirudin TFA

SKU: orb1982180

Description

Bivalirudin TFA, a synthetic 20-residue peptide, serves as a reversible inhibitor of thrombin. Its IC50 value highlights its target specificity in vitro, where, combined with Eptifibatide (8 mg/mL) at a low concentration (70 ng/mL), it significantly reduces platelet aggregation induced by thrombin (0.2 U/mL) by approximately 90%. The compound demonstrates no effect on thrombin generation assay (TGA) parameters up to 10 μmol/L. Additionally, it facilitates the binding of MPO to BAEC, leading to functional alterations such as increased NO consumption and enhanced MPO-mediated redox modifications. In vivo studies reveal its efficacy in preventing the rise of antiheparin/PF4 antibody IgG levels in rats, with significant findings from the toxicokinetic assessment signaling its safety profile at tested doses, although higher doses resulted in fatalities. In clinical trials, its antithrombotic effects were explored, comparing it with alternatives like Ticagrelor and Clopidogrel in a Phase 4 study.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1191386-55-6
• MW: 2294.34
• Formula: C₉₈H₁₃₈N₂₄O₃₃.C₂HF₃O₂
• SMILES: CCC(C)[C@H](NC(=O)C(CCC(O)=O)NC(=O)C(CCC(O)=O)NC(=O)C(Cc1ccccc1)NC(=O)C(CC(O)=O)NC(=O)CNC(=O)C(CC(N)=O)NC(=O)CNC(=O)CNC(=O)CNC(=O)CNC(=O)C1CCCN1C(=O)C(CCCNC(N)=N)NC(=O)C1CCCN1C(=O)C(N)Cc1ccccc1)C(=O)N1CCCC1C(=O)NC(CCC(O)=O)C(=O)NC(CCC(O)=O)C(=O)NC(Cc1ccc(O)cc1)C(=O)NC(CC(C)C)C(O)=O
• Target: Thrombin

Storage & Handling

• Storage: -20°C
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Thrombin