fxia

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.

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

FXIa-IN-14 (Compound 14c) serves as an inhibitor of FXIa, demonstrating potency with an IC50 value of 15 nM [1].

FXIa-IN-1 is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.

FXIa-6f is a high affinity, orally bioavailable macrocyclic FXIa inhibitor with antithrombotic activity in preclinical species

FXIa-IN-13 (example 1), a Factor Xa inhibitor with antithrombotic properties, effectively inhibits arteriovenous thrombosis both in vivo and in vitro [1].

FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most relevant serine proteases (K_i = 0.3 nM), demonstrating excellent pharmacokinetics (PK) profile, including high oral bioavailability and low clearance, in multiple preclinical species.

FXIa-IN-8, a potent and selective inhibitor of FXIa (IC50: 14.2 nM), exhibits anti-thrombotic effects without increasing the risk of bleeding or causing significant toxicity [1].

FXIa-IN-10 is a potent, orally bioavailable inhibitor of Activator XI (FXIa) (Ki: 0.17 nM).

FXIa-IN-9 (compound 3f) is a potent, selective inhibitor of FXIa, demonstrating strong binding affinity through hydrogen bond formation (human FXIa Ki: 0.17 nM, rabbit FXIa Ki: 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].

Milvexian (BMS-986177) is a potent antithrombotic compound that inhibits human and rabbit factor XIa (FXIa) directly and reversibly. It is orally-bioavailable and exhibits a K i of 0.11 nM and 0.38 nM against human and rabbit FXIa, respectively.

BMS-262084 is a potent selective β-lactam trypsin inhibitor with therapeutic potential in the treatment of asthma.

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa) with inhibition constants (Kis) of 0.2 nM for human FXIa and 0.42 nM for rabbit FXIa.

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

FD-IN-1 is a factor D (FD) inhibitor with an IC50 of 12 nM.FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5μM, respectively. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system.

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.

BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1].