Factor Xa Inhibitor

Fitusiran (ALN-AT3SC) sodium is a siRNA strategy. Fitusiran delivers siRNA targeting the SERPINC1 gene in hepatocytes to inhibit antithrombin synthesis. Fitusiran sodium enhances thrombin activity and increases Thrombin generation, thereby restoring hemostatic function. Fitusiran sodium can be used in hemophilia-related research.

Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a K_a of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases.

Rivaroxaban-d₄ (BAY 59-7939-d₄) is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC₅₀ 0.7 nM; K_i 0.4 nM).

Apixaban ethyl ester is a key intermediate in the synthesis of FXa inhibitors, which is used to study the inhibitory activity against venous thrombosis.

Edoxaban M4 (D21-2393) is an orally active and selective Factor Xa inhibitor with a human Factor Xa IC₅₀ of 1.8 nM. Edoxaban M4 exhibits anticoagulant activity via Factor Xa inhibition. Edoxaban M4 can be used for the research of non-valvular atrial fibrillation, venous thromboembolisms, pulmonary embolism.

BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC₅₀ of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC₅₀=5 nM). BMS-262084 exhibits antithrombotic effects.

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.

Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.

Denecimig (Mim8) is a factor VIII-mimetic bispecific antibody with micromolar human binding affinity for Factor X and Factor IXa. Denecimig binds Factor X and Factor IXa, localizes both to the phospholipid surface, enhances the Factor IXa-mediated activation of Factor X to Factor Xa, and stimulates the proteolytic activity of Factor IXa via its monovalent anti-Factor IXa arm. Denecimig is applicable to research related to hemophilia A.

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.

BMS-962212 is a factor XIa (FXIa) inhibitor with a K_i of 0.7 nM against human FXIa and a K_i of 3 nM against rabbit FXIa. BMS-962212 blocks thrombosis while preserving normal hemostatic function. BMS-962212 is applicable to thrombosis-related research.

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.

NCGC00351170 is an antiplatelet agent that disrupts the calcium and integrin-binding protein 1 (CIB1)-α_IIbβ₃ interaction. NCGC00351170 inhibits thrombin-induced human platelet aggregation.

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.

Rivaroxaban (Standard) is the analytical standard of Rivaroxaban. This product is intended for research and analytical applications. Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC₅₀ 0.7 nM; K_i 0.4 nM).

Apixaban (Standard) is the analytical standard of Apixaban. This product is intended for research and analytical applications. Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.

GalNAc unconjugated/naked Fitusiran (sodium), an small interfering RNA without GalNAc conjugation, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia.

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.

Dechloro Rivaroxaban is a highly selective, orally active inhibitor of Factor Xa. Dechloro Rivaroxaban inhibits human free FXa with a K_i of 0.4 nM. Dechloro Rivaroxaban inhibits prothrombinase activity and fibrin-associated FXa activity with IC₅₀s of 2.1 nM and 92 nM, respectively.

Apixaban-¹³C,d₃ (BMS-562247-01-¹³C,d₃) is a deuterium and ¹³C labeled Apixaban (HY-50667). Apixaban is a highly selective, reversible inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively.