fxa

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.

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

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

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.

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.

Edoxaban impurity 6 is an impurity of 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[1][2]. [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.[2]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23.

Concizumab is an anti-TFPI monoclonal antibody (IgG4 type) that selectively binds to the Kunitz protease inhibitor (KPI) 2 domain of TFPI, thereby blocking the interaction of this domain with the FXa active site. Injections of Concizumab increase thrombin in the blood and can be used to prevent and treat hemophilia.

Rivaroxaban D4 is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent,selective and direct inhibitor of Factor Xa (FXa)(IC50:0.7 nM; Ki:0.4 nM).

DX-9065A is a factor Xa inhibitor. DX-9065a inhibits proinflammatory events induced by factor Xa and gingipains. DX-9065a is a competitive inhibitor of the Spectrozyme FXa (SpFXa) cleavage by both fXa and prothrombinase with similar K(i) values of approxi

Methoxycarbonyl-D-Nle-Gly-Arg-pNA is a synthetic trypsin substrate utilized for coagulation factors IXa (FIXa) and Xa (FXa), as evidenced by studies [1] [2] [3].

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

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

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.

YM-60828 dihydrochloride is a Factor Xa (FXa) inhibitor and anticoagulant used in the treatment of venous thromboembolic disease.

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].

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

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 impurity 4, an impurity of Edoxaban (DU-176), is a selective, potent, and orally active inhibitor of factor Xa (FXa), exhibiting Kis of 0.561 nM for free FXa and 2.98 nM for prothrombinase. As an anticoagulant agent, Edoxaban is utilized for stroke prevention[1][2].

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.

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

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

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)

CVS-1578 is a potent serine protease inhibitor, targeting the S2S3 thrombin and FXa subsites.

Otamixaban(FXV673) is an effective (Ki = 0.5 nM), selective, rapid-acting, competitive, and reversible fXa inhibitor. It also effectively inhibits both free and prothrombinase-bound fXa.

GW-813893 is a potent, selective and orally active factor Xa inhibitor. GW813893 inhibited FXa and prothrombinase activity with a Ki of 4.0 nM and 9.7 nM, respectively.

Edoxaban (DU-176b) hydrochloride is a potent, selective, orally active, direct inhibitor of Factor Xa (FXa), acting on human free FXa (Ki: 0.561 nM) and thrombinogenase (Ki: 2.98 nM). Edoxaban hydrochloride is more than 10,000 times more selective than other thrombinases and can be used in studies to prevent thromboembolic disease.

APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.

BMS-344577, a lactam derivative based on arylguanidine, is a potent oral active FXA inhibitor with excellent susceptibility in vitro, good pharmacokinetics, and pharmacodynamics in animal models.

Rivaroxaban (BAY 59-7939) is an orally bioavailable oxazolidinone derivative and direct inhibitor of the coagulation factor Xa with anticoagulant activity. Upon oral administration, rivaroxaban selectively binds to both free factor Xa and factor Xa bound in the prothrombinase complex. This interferes with the conversion of prothrombin (factor II) to thrombin and eventually prevents the formation of cross-linked fibrin clots. Rivaroxaban does not affect existing thrombin levels.

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

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

Edoxaban-d6 is a deuterated compound of Edoxaban. Edoxaban has a CAS number of 480449-70-5. Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.