Factor Xa

EMD-503982 is a potential Factor Xa and Factor VIIa inhibitor with potential anticancer and antitumor activity for the study of thromboembolic and neurological disorders.

Fondaparinux sodium (SR-90107A) is an antithrombin-dependent factor Xa inhibitor with antithrombotic activity.

Abelacimab (MAA868), a fully human IgG1 monoclonal antibody that binds to and blocks the activation of FXI, is an anticoagulant used in the study of thromboembolic diseases.

Asundexian (BAY-2433334) is a potent and orally active inhibitor of the coagulation factor FXIa that directly and reversibly binds to the active site of FXIa, thereby inhibiting its activity.Asundexian has an IC50 of 1 nM for human FXIa in buffer.Asundexian has antitumor activity and may be useful in studies of Acute ischemic stroke, transient ischemic attack and ischemic stroke.

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.

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.

Garadacimab (CSL312) is a potent whole-human IgG4 monoclonal antibody targeting activation factor XII (FXIIa). Garadacimab can be used to study hereditary angioedema.

Eribaxaban (PD348292) is an orally available factor Xa inhibitor for the prevention and treatment of venous thromboembolism.

Denecimig (Mim8) is a bispecific and humanized IgG4κ antibody mimicking activated coagulation factor VIII with anti-FIXa and anti-FX arms, which is used for the treatment of hemophilia A and coagulation disorders primarily by facilitating the assembly of activated coagulation factors IXa (FIXa) and X (FX) on platelet membranes, stimulating activation of FX, and arresting bleeding.

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.

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].

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.

LY 517717 is an orally active inhibitor of coagulation factor Xa with antithrombotic activity for the study of venous thromboembolism (VTE).

Otamixaban (FXV673) is a selective and highly effective Xa inhibitor that inhibits the generation of thrombin and can be used to study acute coronary syndrome.

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].

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

Coumarin is a chemical compound poison found in many plants, notably in high concentration in the tonka bean, woodruff, and bison grass. It has clinical value as the precursor for several anticoagulants, notably warfarin.

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.

Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate has an inhibitory effect on coagulation factor Xa, and it can be used in the study of thrombophlebitis, atherosclerosis, cerebral embolism, stroke and pulmonary embolism.

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.

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.

4-Chlorophenylurea (NSC-12971) is a novel orally bioavailable inhibitor of factor Xa.

2-Methoxy Phenothiazine is light yellow or light gray solid.

Letaxaban (TAK-442) is a small molecule Xa factor inhibitor that can be used to study polar coronary syndromes and thrombotic blockages.

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

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

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

FXIa-IN-7 is an orally available, selective and potent factor XIa inhibitor for the study of thrombophilia.

Rivaroxaban-d4 is a deuterated marker of Rivaroxaban 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.

FXIa-IN-15 (Compound (S)-10h) is an inhibitor of factor XIa (FXIa) and plasma kallikrein (PKa) with IC50 values of 0.38 nM and 59.2 nM, respectively. It exhibits anticoagulant properties by prolonging the 50% activated partial thromboplastin time (aPTT) with an EC1.5X of 0.55 μM.

D-Pro-Phe-Arg-Chloromethylketone, an inhibitor of coagulation factor XII and plasma kallikrein, is significant in the regulation of thrombosis and inflammation [1].

cMCoFx1 is an effective and selective FXIIa cyclic peptide inhibitor. It exhibits high binding affinity for FXIIa (KD: 900 pM) and potent inhibitory activity (Ki: 370 pM). cMCoFx1 effectively suppresses the intrinsic coagulation pathway, demonstrates high stability in serum, and shows no cytotoxicity.

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.

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

CH3OCO-D-CHA-Gly-Arg-pNA acetate is a documented chromogenic substrate for Factor Xa, as noted in sources [1] [2].

Frunexian (EP-7041) is a selective, potent inhibitor of coagulation factor XI activated factor XI, specifically targeting XIa. It shows antithrombotic activity without bleeding risk in a rat mesenteric arterial puncture model and is applicable in extracorporeal membrane oxygenation (ECMO) research [1].

Lofacimig is a bispecific antibody of VH-VH-G1(h-CH2-CH3) dimer type that targets FXI PTA.