factor xa (human)

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.

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.

Apixaban 13C,d3 is a deuterium labeling of Apixaban for isotopic tracing. Apixaban 13C,d3 is a selective inhibitor of coagulation factor Xa and is used in thromboembolism studies

O-Desmethyl apixaban is a metabolite of Apixaban and a highly selective, reversible inhibitor of Factor Xa, with Ki values of 0.08 nM in humans and 0.17 nM in rabbits.

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

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.

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.

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.

Edoxaban (DU-176b) hydrochloride is a potent, selective, orally active, direct inhibitor of Factor Xa (FXa), targeting human free FXa (Ki: 0.561 nM) and thrombinogenase (Ki: 2.98 nM). Over 10,000 times more selective than other thrombinases, it is suitable for studies to prevent thromboembolic disease.