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Thrombin inhibitors block the serine protease that converts fibrinogen into fibrin at the end of coagulation. Thrombin also activates platelets and other cells through protease-activated receptors (PARs). The receptor cloned in 1991 showed that thrombin cleaves the receptor N-terminus and unmasks a tethered ligand. Direct inhibitors bind the active site and are used in coagulation, platelet and vascular research. Dabigatran came from a structure-based design program reported in 2002, and dabigatran etexilate is its orally available prodrug. Argatroban, bivalirudin, inogatran and ximelagatran are further direct thrombin inhibitors. Atopaxar hydrobromide acts on the receptor side as a PAR-1 antagonist, whereas RWJ-445167 inhibits both thrombin and factor Xa.
Synonyms: BIBR 953; Pradaxa
BIBR 953 (Dabigatran, Pradaxa) is a highly selective, reversible, and potent thrombin inhibitor and is orally available as the prodrug, dabigatran etexilate. It has shown antithrombotic efficacy in animal models of thrombosis, with a rapid onset of action and predictable pharmacodynamic response.
Synonyms: BIBR-1048
BIBR-1048 (Dabigatran etexilate) is an anticoagulant from the class of the direct thrombin inhibitors.
Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.
Synonyms: 3DP-10017
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
Synonyms: H 37695
Ximelagatran is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy.
Synonyms: H-314-27
Inogatran (H-314-27) is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
Synonyms: BG-8967
Bivalirudin is a synthetic 20 residue peptide which reversibly inhibits thrombin.
Synonyms: Pradaxa; BIBR 1048MS; Dabigatran etexilate methanesulfonate
Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.
Dabigatran ethyl ester, which is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity.
Synonyms: D-Phe-Pro-Arg-CMK
PPACK is a potent, selective and irreversible inhibitor of thrombin with a Ki value of 0.24 nM.
Synonyms: MD-805 monohydrate; MCI-9038 monohydrate
Argatroban monohydrate is a direct and selective inhibitor of thrombin. It plays a critical role in anticoagulation therapy, particularly for patients with heparin-induced thrombocytopenia. Argatroban is widely used in research to study coagulation pathways and evaluate potential therapeutic approaches for thrombotic disorders.
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin.
Synonyms: DS1040
DS-1040 Tosylate is an inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa), used for the treatment of acute ischemic stroke (AIS).
Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor.
Synonyms: SB-424323
Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.
Hirudin is a potent thrombin inhibitor known for its anticoagulant properties. It exhibits significant anti-thrombotic activity and is implicated in therapeutic applications such as wound repair, anti-fibrosis, and anti-tumor responses. Additionally, Hirudin has been explored for its effects on diabetic complications and cerebral hemorrhage, making it a valuable reagent in various research contexts.
Synonyms: Cacticin
Isorhamnetin 3-O-galactoside is a flavonoid glycoside that acts as a thrombin inhibitor, isolated from Oenanthe javanica. It exhibits significant antithrombotic and profibrinolytic properties by inhibiting thrombin and factor Xa activity, thereby reducing the maximum rate of thrombin-catalyzed fibrin polymerization. Additionally, Isorhamnetin 3-O-galactoside suppresses TNF-α-induced PAI-1 secretion and decreases the PAI-1/tissue-type plasminogen activator (t-PA) ratio, making it instrumental in research on liver injury and thrombotic vascular diseases.
5-((1H-Indol-3-yl)methylene)imidazolidine-2,4-dione is a potent inhibitor of the dengue virus NS2B-NS3 protease and thrombin. This compound is valuable for studying the mechanisms of viral replication and coagulation processes, making it an essential tool in research focused on infectious diseases and related therapeutic interventions. Its dual activity highlights its potential for investigating the dynamics of viral pathology and thrombotic complications.
Synonyms: PER977
Ciraparantag is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants. This compound effectively neutralizes the effects of low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. Its unique mechanism makes Ciraparantag a valuable tool for research focused on anticoagulation reversal and hemostasis.
Synonyms: PER977 acetate
Ciraparantag acetate is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants, including low molecular weight heparins, unfractionated heparins, and certain direct oral anticoagulants, excluding vitamin K antagonists (VKAs). Its primary mechanism targets the coagulation pathway, facilitating the restoration of normal hemostasis in clinical situations where anticoagulation reversal is necessary. Ciraparantag acetate is valuable in research applications focused on anticoagulation management and hemostatic balance in cardiovascular studies.
Synonyms: PER977 TFA
Ciraparantag TFA is a potent thrombin and factor Xa inhibitor utilized as a broad-spectrum reversal agent for anticoagulants. It effectively antagonizes the effects of various anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and specific direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. This compound is significant for research applications focused on enhancing hemostatic management in patients receiving anticoagulant therapy.
Synonyms: Thiolstatin D
Bacithrocin D is a potent inhibitor of key proteases, specifically targeting thrombin, factor Xa, trypsin, and papain. It effectively prolongs clotting time, making it valuable in studies related to coagulation and hemostasis. Bacithrocin D demonstrates IC50 values of 124 μM for thrombin, 9 μM for factor Xa, 0.85 μM for trypsin, and a remarkable 0.01 μM for papain, showcasing its high potency against these proteases. This reagent is useful for investigating protease-related pathways and developing therapeutic strategies in anticoagulation research.
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Bacithrocin A is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain, demonstrating IC50 values of 48 μM, 13 μM, 0.65 μM, and 0.02 μM, respectively. This compound is of particular interest in the study of coagulation processes and the development of anticoagulant therapies. Its broad-spectrum inhibitory activity makes it a valuable reagent for biological research focused on protease activity modulation and hemostasis.
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