fxia-in-1

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

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

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

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-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].

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.