factor xa

Iptacopan (LNP023) is an inhibitor with high affinity for factor B.

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.

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.

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

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

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

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

Rivaroxaban Impurity (Rivaroxaban-10) is a potent Blood-coagulation factor Xa inhibitor, IC50= 66 nM.

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.

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.

Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.1 Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.References1. Aruell, L., Friberger, P., Karlsson, G., et al. A new sensitive and highly specific chromogenic peptide substrate for factor Xa. Thromb. Res. 11(5), 595-609 (1977). Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.1 Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity. References1. Aruell, L., Friberger, P., Karlsson, G., et al. A new sensitive and highly specific chromogenic peptide substrate for factor Xa. Thromb. Res. 11(5), 595-609 (1977).

Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride is a chromogenic substrate specifically designed for factor Xa.

Thrombin is a trypsin-like serine protease that is encoded by the F2 gene in humans. Thrombin is produced by the enzymatic cleavage of two sites on prothrombin by activated Factor X (Xa). Thrombin in turn acts as a serine protease that converts soluble

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.

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).

Ciraparantag TFA is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.

DJT06001 is a selective Factor Xa inhibitor, reducing thrombus formation with low risk of bleeding.

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

Idraparinux Na is an Antithrombotic, Indirect, Selective, Synthetic Factor Xa Inhibitor

GCC-4401C methanesulfonate is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).

GGACK is an inhibitor of urokinase-type plasminogen activator (uPA) and factor Xa (Kis = 1.8 and 8.7 μM, respectively).1,2 1.Kettner, C., and Shaw, E.The susceptibility of urokinase to affinity labeling by peptides of arginine chloromethyl ketoneBiochim. Biophys. Acta569(1)31-40(1979) 2.Kettner, C., and Shaw, E.The selective affinity labeling of factor Xa by peptides of arginine chloromethyl ketoneThromb. Res.22(5-6)645-652(1981)

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

KFA1982 is a novel and potent factor Xa inhibitor.

Darexaban glucuronide is the major component in plasma after oral administration of darexaban to humans. Darexaban (YM150) is a direct inhibitor of factor Xa.

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with K i s of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa , Thrombin and tPA, respectively [1] [2] .

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).

p-APMSF is an irreversible inhibitor of serine proteases with Ki values of 1.02, 1.18, 1.5, and 1.54 μM for bovine trypsin, human thrombin, bovine plasmin, and bovine Factor Xa, respectively. It is selective for these proteases over bovine chymotrypsin and acetylcholinesterase.

Edoxaban Isomer is an impurity of Edoxaban, which is a novel inhibitor of factor Xa.

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

BI-11634 is a factor Xa inhibitor.

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

O-Desmethyl apixaban is a metabolite of Apixaban that is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

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.

PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.

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].

Z-RGR-pNA is a chromogenic substrate for the determination of factor Xa.

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].

Ciraparantag is an inhibitor of thrombin and factor Xa. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including unfractionated heparin, low-molecular-weight heparin, and certain direct oral anticoagulants.

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.

Boc-Ile-Glu-Gly-Arg-AMC (IEGR-AMC), a specific, highly fluorogenic substrate for clotting enzyme factor Xa (coagulation factor Xa). Boc-IEGR-AMC is also hydrolyzed by acrosin from the ascidian Halocynthia roretzi.

ARC19499, an aptamer, inhibits the tissue factor pathway inhibitor (TFPI), facilitating clot initiation and propagation through the extrinsic pathway. It binds specifically to TFPI, blocking its inhibition of both factor Xa and the TF/factor VIIa complex, thereby correcting thrombin generation in hemophilia A and B plasma and restoring clotting in FVIII-neutralized whole blood.

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)

O-Demethyl apixaban sulfate is a metabolite of Apixaban, a potent and highly selective factor Xa inhibitor. Apixaban is currently under development for treatment of arterial and venous thrombotic diseases.

JTV-803 is a factor Xa inhibitor. JTV-803 showed a competitive inhibitory effect on human factor Xa, with a K(i) value of 0.019 microM and IC(50) value of 0.081 microM. JTV-803 was 100 times more selective in inhibiting human factor Xa as compared to its

Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium-labeled Apixaban. Apixaban is a reversible inhibitor of Factor Xa (Ki: 0.08 nM and 0.17 nM in human and rabbit).