Thrombin Inhibitor

Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.

Edoxaban (DU-176b) monohydrate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K_is of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban monohydrate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban monohydrate can be used for preventing thromboembolic disease research.

PPACK dihydrochloride is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK dihydrochloride specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK dihydrochloride exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK dihydrochloride binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK dihydrochloride is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases.

Isovanillic acid (3-Hydroxy-4-methoxybenzoic acid) is a phenolic acid isolated from isolated from Scrophularia ningpoensis, with anti-thrombotic activity.

Dabigatran ethyl ester is an inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) and thrombin. Dabigatran ethyl ester inhibits NADH-dependent metabolism of mitomycin C mediated by purified recombinant human NQO2.

Anisindione is an oral indandione anticoagulant. Anisindione inhibits the formation of active procoagulant factors II, VII, IX and X. Anisindione can be used in anticoagulation-related research.

Heparin (Nadroparin) calcium (MW 3600-5000) is an anticoagulant which binds reversibly to antithrombin III (ATIII) to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors IX, X, XI, and XII and prevents the transformation of fibrinogen to fibrin.

DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC₅₀s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.

Ciraparantag (PER977) is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban.

Isorhamnetin 3-O-galactoside (Cacticin) is a flavonoid glycoside that can be isolated from Oenanthe javanica, with antithrombotic and profibrinolytic activities. Isorhamnetin 3-O-galactoside inhibits the activities of thrombin and factor Xa (FXa) and reduces thrombin-catalyzed fibrin polymerization maximum rate. Isorhamnetin 3-O-galactoside suppresses TNF-α-induced PAI-1 secretion, decreases the PAI-1/tissue-type plasminogen activator (t-PA) ratio, and inhibits FXa production and FVa/FXa-mediated thrombin generation. Isorhamnetin 3-O-galactoside exerts protective effects against Carbon tetrachloride (CCl4) (HY-Y0298)-induced hepatic injury in mice. Isorhamnetin 3-O-galactoside can be used for the study of liver injury-related diseases and thrombotic vascular diseases.

Odiparcil (SB-424323) is an orally active β-D-xyloside derivative. Odiparcil can effectively divert the synthesis of cellular glycosaminoglycans (GAG) into secreted soluble species and reduce GAG accumulation. Odiparcil shows antithrombin and antiplatelet activity. Odiparcil can be used for the researches of metabolic and cardiovascular disease, such as mucopolysaccharidoses (MPS) and thrombosis.

FXIIa-IN-4 (compound 22) is a potent, selective human FXIIa inhibitor with the IC₅₀ of 0.032 μM, 0.30 μM, ＞50 μM for FXIIa, thrombin and FXIa, respectively. FXIIa-IN-4 can be used for study of anticoagulant.

Dabigatran-d₃ is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC₅₀=10 nM).

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 also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.

Befovacimab (BAY 1093884) is a fully human monoclonal IgG2 antibody able to bind to tissue factor pathway inhibitor (TFPI). Befovacimab can be used for haemophilia A/B research.

Metolazone (Standard) is the analytical standard of Metolazone. This product is intended for research and analytical applications. Metolazone (SR-720-22) is primarily used to treat congestive heart failure and high blood pressure.

NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca²⁺ inward flow.

Melagatran is a reversible, selective, orally active direct inhibitor of thrombin with a K_i of 2 nM. Melagatran binds directly to the active site of thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin. Melagatran reduces the DNA binding activity of NF-κB and AP-1. Melagatran reduces fibrin deposition in organs, alleviates ischemic brain damage, and reduces the size of advanced atherosclerotic lesions. Melagatran can be used in the study of cardiovascular disease (coronary thrombosis, atherosclerosis) and ischemic brain damage.

Edoxaban (DU-176b) tosylate is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K_is of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban tosylate exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban tosylate can be used for preventing thromboembolic disease research.