Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor.
Idraparinux (sodium) is a polymethylated synthetic pentasaccharide known to interact with the antithrombin III and act as anticoagulant.
TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
Sar-Pro-Arg-pNA is a chromogenic substrate of α-thrombin. Sar-Pro-Arg-pNA can be used to test α-thrombin activity[1].
Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide, and has high affnity for thrombin than Hirugen, with a KD < 100 nM. Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is an antithrombotic agent. Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) inhibits the thrombin-induced fibrin clot formation with an IC50 value of 0.087 μM[1].
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics[1][2].
OM-189 is a selective synthetic thrombin inhibitor.
Hirudin is a Thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others[1].
Desethyl KBT-3022 is the main active metabolite of the new antiplatelet agent, KBT-3022.
Argatroban is a direct, selective thrombin inhibitor.Target: ThrombinArgatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries [1]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban [2].
Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity[1].
Melagatran is a direct and oral active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia[1]. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion[2].
Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein[1][2][3].
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1].
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT)[1].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].
NQ301 is an antithrombotic agent; inhibits collagen-challenged rabbit platelet aggregation with an IC50 of 10 mg/mL.
RWJ-445167 is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
Inogatran is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
Hirullin P18 is a potent thrombin inhibitor. Hirullin P18 has an anticoagulant effect[1].
Rovunaptabin (ARC 183) is a DNA aptamer, which is a single-stranded DNA molecule consisting of 15 deoxynucleotides that forms well-defined three-dimensional configuration, allowing it to bind to thrombin with high affinity and specificity.
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) [1][2].
Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.