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Bivalirudin TFA

CAS No. : 1191386-55-6

Biological Activity：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

Research Area：Cardiovascular Disease

Targets：Thrombin

Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;Bioactive Compound Library Plus;Peptide Library;

Related Small Molecules:OM-189;Thrombin Inhibitor 2;Razaxaban hydrochloride;Desethyl KBT-3022;Idraparinux sodium;TP508;Inogatran;RWJ-445167;Napsagatran hydrate;BAY 1217224;Thrombin (MW 37kDa);Ximelagatran-d11;Melagatran;(1R,3S)-THCCA-Asn;Sfllrnpndkyepf

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