Thrombin
Thrombin is a Na+ -activated allosteric serine protease that catalyzes the formation of thrombus as well as a series of flux-regulating reactions through the coagulation cascade. In response to vascular injury, thrombin is produced through the activation of its inactive precursor, prothrobin, catalyzed by Factor Xa (a trypsin-like proteinase). As a serine protease characterized by the presence of a catalytic triad, thrombin possess a triad of S195-H57-D189 in its active center, which is required for the nucleophilic attack of the target peptide bond. Located “south-west” of the active center is a Na+ -binding site, through which the binding of a sodium ion allosterically modulates the activity of the serine proteinase.
- C4021 TS 155-2Summary: macrocyclic lactone that inhibits thrombin-stimulated calcium entry into cells
- A8363 ArgatrobanSummary: Thrombin mediated fibrinogen cleavage inhibitor
- A8381 BIBR-1048Summary: Thrombin inhibitor
- A5066 Heparin sodiumSummary: Antithrombin III activator
- A4077 BIBR 953 (Dabigatran, Pradaxa)Summary: Thrombin inhibitor,potent,reversible and direct
- A2588 PPACK DihydrochlorideSummary: Thrombin inhibitor
- A4341 ApixabanSummary: Factor Xa inhibitor
- A3126 5-R-RivaroxabanTarget: Factor XaSummary: Factor Xa (FXa) inhibitor
- A3244 Bivalirudin TrifluoroacetateTarget: thrombinSummary: Reversible thrombin inhibitor
- A3345 Dabigatran etexilate mesylateSummary: Direct thrombin inhibitor,anticoagulant,prodrug of dabigatran