thrombin

Thrombin inhibitor 1 is a potent inhibitor of thrombin [Ki: 0.66 nM, 2xaPTT=0.43 μM].

Thrombin (MW 37kDa) is an allosteric serine protease with trypsin-like activity.

Melagatran is an orally available, direct synthetic thrombin inhibitor that does not require endogenous cofactors other than thrombin and does not significantly interact with any other enzymes in the coagulation cascade or with the fibrinolytic enzymes.

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

Menadione (Vitamin K3) is a synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Edoxaban (Lixiana) (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

Protamine sulfate is a polycationic peptide compound with anti-heparin activity. It can neutralize the anticoagulant effects of heparin, enhance lipid-mediated gene transfer, and is commonly used to establish cystitis models.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

AEBSF hydrochloride (Pefabloc SC) is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, thrombin, plasmin, and trypsin.

Heparin sodium is a sulfated polysaccharide, which belongs to the family of glycosaminoglycans. It is utilized as an anticoagulant and interacted with diverse proteins for numerous important biological activities.Heparin sodium salt (Sodium heparinate) significantly inhibits exosome-cell interactions.

Argatroban is a specific thrombin inhibitor and a non-heparin anticoagulant that effectively prevents thrombus formation and is commonly used to establish thrombolysis models.

Dabigatran ethyl ester hydrochloride is an effective inhibitor of ribosyl dihydronicotinic acid amide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and is a thrombin inhibitor.

OM-189 is a selective inhibitor of synthetic thrombin.

Razaxaban hydrochloride is a highly potent, selective and orally active inhibitor of factor Xa(Ki of 0.19 nM),has strongly antithrombotic activity.

RWJ-445167 is a thrombin and factor Xa dual inhibitor(Ki of 4.0 nM and 230 nM, respectively), with potent antithrombotic activity.

Dabigatran ethyl ester (Dabigatran (ethyl ester)) is an emerging oral anticoagulant and it also is a direct inhibitor of thrombin activity.

Metolazone (SR-720-22) is a quinazoline-sulfonamide derived diuretic that inhibits sodium chloride symporters.

Napsagatran hydrate is a novel and specific thrombin inhibitor.

Odiparcil is an orally active beta-d-thioxyloside analog. Odiparcil is an indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II). It also has an antithrombotic activity associated with a reduced risk of adverse bleeding events.

Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor with antithrombotic activity.

Ximelagatran (H 376-95), a direct thrombin inhibitor, can be taken orally and acts solely by inhibiting the actions of thrombin. Ximelagatran is converted to the active agent melagatran in vivo.

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.