Thrombin

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor, which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation.

Dabigatran prevents blood clots, inhibiting NQO2 and thrombin with IC50 0.8 μM.

Bivalirudin acetate is a thrombin inhibitor, a peptide-based anticoagulant, used for research on acute coronary syndrome.

Hirullin P18 is a potent thrombin inhibitor with anticoagulant properties [1].

Hirudin (55-65) (sulfated), a fragment of Hirudin, is a thrombin inhibitor with anticoagulant effects and blood anticoagulant properties.

Thrombin receptor peptide ligand, a thrombin receptor antagonist, serves as an antithrombotic agent [1].

Knob A peptide GPRPFPAC is a fibrin knob peptide. The PEGylated form of Knob A peptide GPRPFPAC exhibits enhanced anticoagulant activity.

Fibrinogen-binding peptide mimics vitronectin site and activates platelets; thrombin turns it to fibrin.

YD-3 is a PAR4 antagonist that significantly inhibits thrombin-induced platelet aggregation in rabbits (IC(50)=28.3 microM). In addition, YD-3 suppresses thrombin-induced proliferation of vascular smooth muscle cells (VSMCs) and reduces neointimal thickening after balloon injury. Through Ras- and ERK1/2-mediated signaling pathways, YD-3 impedes thrombin-driven VSMC proliferation. When analyzed with Western blot, YD-3 primarily inhibits thrombin-induced expression of vascular endothelial growth factor receptor 2 (Flk-1) without affecting extracellular signal-regulated kinase 1/2 phosphorylation. YD-3 could potentially have value in elucidating the pathophysiology of thrombin-induced angiogenesis.

A unique collection of 343 protease and proteasome inhibitors for research in chemical genomics, and drug screening;

Sulodexide is an orally administered combination of glycosaminoglycans, consisting of low molecular weight heparin (80%) and dermatan sulfate (20%). It demonstrates antithrombotic properties by interacting with antithrombin III (AT III) and heparin cofactor II (HC II), and by inhibiting thrombin formation. Additionally, sulodexide enhances profibrinolytic activity by releasing tissue plasminogen activator (tPA). It also offers endothelial protection, possesses anti-inflammatory effects, and alleviates chronic venous disease.

Fibrinopeptide B (FPB) is produced during the cleavage of fibrinogen, by thrombin, to fibrin monomer.

Platelet aggregation-IN-1 (Compound 10e) acts as an inhibitor of platelet aggregation and can achieve complete (100%) inhibition of thrombin-induced platelet aggregation at a concentration of 50 μM.

Thrombin inhibitor 13 (Compound 13a) acts as a covalent reversible inhibitor of thrombin (thrombin, FIIa) with an IC50 of 0.7 nM. This compound prolongs activated partial thromboplastin time (aPTT) and prothrombin time (PT), demonstrating both antithrombotic and anticoagulant properties.

Ichorcumab (JNJ-375) is a fully human IgG4 antibody that targets thrombin. It binds to exosite 1 of thrombin, inhibiting substrate binding without affecting its catalytic activity. For isotype control, refer to HumanIgG1kappa, Isotype Control.

H-Gly-Arg-pNA 2HCl, a peptide, binds 1,2 thrombin; colorimetric quantification at 405 nm indicates thrombin activity.

Peptide that reverses the anticoagulant effect of heparin. Potently binds heparin (Kd = 36 nM in vitro).

Thrombin (MW 37kDa) is a trypsin-like allosteric serine protease.

Hirudin (54-65) TFA, a segment of the 65-amino-acid protein Hirudin, exhibits anticoagulant properties [1].

Acetyl-Hirudin (54-65) (sulfated) binds thrombin-rHCII(L444R), blocking rHCII's N-terminal/thrombin exosite I interaction, stabilizing the complex.