fxa

Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

Apixaban (BMS-562247-01) is an orally active anticoagulant that inhibits coagulation factor Xa, directly preventing the conversion of prothrombin to thrombin and the formation of cross-linked fibrin clots.

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

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

5-R-Rivaroxaban is the (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective direct Factor Xa (FXa) inhibitor with an IC50 of 0.7 nM and a Ki of 0.4 nM.

Rivaroxaban (BAY 59-7939) is an orally bioavailable oxazolidinone derivative and a direct inhibitor of coagulation factor Xa with anticoagulant activity. Upon administration, it selectively binds to both free factor Xa and factor Xa within the prothrombinase complex, interfering with the conversion of prothrombin (factor II) to thrombin and preventing cross-linked fibrin clot formation. Rivaroxaban does not affect existing thrombin levels.

Enoxaparin sodium is a low-molecular-weight heparin (LMWH) that has recently been approved by the US FDA for use in patients with medically managed ST-segment myocardial infarction (STEMI), or STEMI with subsequent percutaneous coronary intervention (PCI)

Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.

Fondaparinux sodium (Arixtra, SR-90107A) is a synthetic heparin anticoagulant and an antithrombin-dependent factor Xa inhibitor (IC50=1909 nM), with high selectivity, low immunogenicity, and favorable pharmacokinetic properties, used for the prevention and treatment of thrombotic diseases.

Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].

FXa-IN-1 is an FXa inhibitor with an IC50 value of 3 nM and a Ki value of 0.7 nM that exhibits good oral bioavailability and half-life (in vivo) and can be used to study thromboembolic diseases.

Zifaxaban (TY-602) is an orally active, competitive and selective inhibitor of factor Xa (FXa) with an IC50 of 11.1 nM for human FXa.Zifaxaban has a very high affinity, more than 10,000-fold higher than that of other serine proteases.Zifaxaban can be used to study arterial and venous thrombosis.

Rivaroxaban-D4 is a deuterated marker of Rivaroxaban (T1184) for isotopic tracing.Rivaroxaban (BAY 59-7939) is a highly potent and selective direct inhibitor of coagulation factor Xa (FXa), with an IC50 = 0.7 nM and a Ki of 0.4 nM.

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

O-Desmethyl apixaban sulfate sodium inhibits factor X (FXa) with a Ki of 58 μM,and is a major circulating metabolite of Apixaban in humans.

SSR-182289A (Free) is a thrombin inhibitor.

APC-6860 is a trypsin-like serine protease inhibitor with \( k_i \) values of 0.21, 0.44, 1.5, 16.8, 20, and 30 μM for uPA, trypsin, tryptase, tPA, thrombin, and factor Xa, respectively. It exhibits a selectivity ratio for tPA versus uPA of 80 and has \( k_i \) values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be utilized for cancer research.

Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) is a potent, selective, and orally efficacious factor Xa (fXa) inhibitor (IC50: 1.5 nM).

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

EMD-503982 is an orally active, direct factor Xa (FXa) inhibitor that also exhibits inhibitory activity against factor VIIa, and has potential antithrombotic, anticancer, and neuroprotective effects. EMD-503982 can be used in research on thrombotic diseases.

Fidexaban (CI1031) is a novel, potent, selective and orally active factor Xa inhibitor that has demonstrated antithrombotic activity in a variety of assays

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].

Dechloro Rivaroxaban is an orally active and highly selective Factor Xa inhibitor.Dechloro Rivaroxaban has a significant inhibitory effect on free FXa in humans.Dechloro Rivaroxaban also has an inhibitory effect on thrombospondin and fibrin-associated FXa activity.

Betrixaban-D6 is a deuterium-labeled Betrixaban. Betrixaban (T4341) is a selective and orally efficacious FXa inhibitor.