thromboembolic

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.

Osocimab (BAY 1213790) is a potent anti-FXIa antibody with a Ki value of 2.4 nM and an EC50 value of 0.2 nM.Osocimab may reduce thrombosis through FXI inhibition.Osocimab is often used as an XI factor inhibitor, has an inhibitory effect on thrombin generation, has an anticoagulant effect, and is used in the study of thromboembolic diseases. Thromboembolic Diseases

AZD1283 is an effective P2Y12 receptor antagonist (EC50: 3.0 ug/kg/min, binding IC50: 11 nM). AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses induced the increase in bleeding time at 33 and 100 μg/kg/min for 3- and 13-fold, respectively. Thus, the therapeutic index (TI) was ≥10 for both compounds.

Abelacimab (MAA868), a fully human IgG1 monoclonal antibody, targets and binds with high affinity to FXI's catalytic structural domain. This interaction ensures FXI remains in its zymogen form, effectively inhibiting activation by FXIIa or thrombin. Such a mechanism underscores Abelacimab's potential application in thromboembolic disease research [1] [2].

Jujuboside B has potent inhibitory effects on collagen-, thrombin-, AA-, and ADP-induced aggregation, and also exhibits superior protection on the thromboembolic model.

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

DS-1040 Tosylate is an oral active, selective thrombolytic inhibitor with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa, is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM

Efegatran, also known as GYKI-14166, RGH-2958 and LY294468, a thrombin inhibitor which is being developed by IVAX for the potential treatment of thromboembolic disorders.

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

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.

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].

Cyproheptadine is a potent and orally active antagonist of the 5-HT 2A receptor. Cyproheptadine has antidepressant and antiserotonergic effects. Cyproheptadine also has antiplatelet and thromboprotective activities that can be used in thromboembolic disorders research [1] [2].

FXIa-IN-9 (compound 3f) is a potent, selective inhibitor of FXIa, demonstrating strong binding affinity through hydrogen bond formation (human FXIa K i : 0.17 nM, rabbit FXIa K i : 0.5 nM). It exhibits anticoagulant properties, making it valuable for research into thromboembolic conditions, including atrial fibrillation, stroke, myocardial infarction, deep vein thrombosis, and pulmonary embolism [1].

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

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.