fxia

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

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

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-16 (Compound 43) is an orally active and selective FXIa inhibitor with an IC50 of 0.19 nM. It demonstrates significant anticoagulant and antithrombotic properties and exhibits a good safety profile in mice. FXIa-IN-16 is applicable in research related to thrombosis treatment.

FXIa-IN-17 (Compound FE12) is a selective FXIa inhibitor with an IC50 of 4.4 nM. It effectively inhibits thrombosis.

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

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].

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].

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

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.

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

Milvexian (BMS-986177/JNJ-70033093) is an orally bioavailable, small-molecule, reversible, and direct antagonist of Factor XIa (FXIa). It exhibits potent inhibitory activity across species, with Ki values of 0.11 nM for human, 0.38 nM for rabbit, and 0.64 nM for dog. By targeting FXIa, Milvexian selectively inhibits the intrinsic pathway of the coagulation cascade. It demonstrates robust antithrombotic efficacy in various in vitro and in vivo models while maintaining a favorable safety profile regarding bleeding risk. It is a critical tool for investigating novel anticoagulant strategies in thrombosis and cardiovascular research.

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.

FD-IN-1 (Compound 12) is an orally active Factor D (FD) inhibitor (IC50=12 nM) that also inhibits Factor XIa (FXIa) and Tryptase β2 with IC50 values of 7.7 and 6.5 μM, respectively.

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].

FXIIa-IN-3 (Compound 8) is an effective and selective inhibitor of Factor XIIa (FXIIa), with an IC50 of 0.045 μM. It demonstrates significant selectivity over related serine proteases, including FXIa, FXa, and FIXa. FXIIa-IN-3 is suitable for research in thromboembolic diseases.

FXIIa-IN-4 (compound 22) is a potent and selective human FXIIa inhibitor, exhibiting IC50 values of 0.032 μM for FXIIa, 0.30 μM for thrombin, and >50 μM for FXIa. It is utilized in anticoagulant research.

Factor XI-IN-2 is a Factor XI activation inhibitor with an IC50 of 20 nM. It does not directly inhibit the enzymatic activity of FXIa but specifically binds to the FXI zymogen, allosterically inhibiting the activation process of the FXI zymogen by FXIIa. Factor XI-IN-2 suppresses thrombosis in a rabbit arteriovenous (AV) shunt thrombosis model and can be used in antithrombotic research.

Feniralstat (compound 30) hydrochloride is a pyrazole derivative and an effective inhibitor of kallikrein, exhibiting an IC50 of 6.7 nM against human plasma kallikrein (pKal). It shows no inhibitory effects on human KLK1, FXIa, or factor XIIa, with IC50 values exceeding 40 μM for each.

Neutrophil elastase-IN-7 (Compound 12) is a potent inhibitor of human neutrophil elastase (HNE) with an IC50 of 0.54 μM. It also exhibits significant inhibitory activity against various coagulation proteins, with IC50 values of 8.2 μM for thrombin, 12.7 μM for FXa, 1.2 μM for FXIa, and 5.7 μM for FXIIIa. Neutrophil elastase-IN-7 is applicable in the study of inflammation, innate immune responses, and tissue remodeling.

D-Leu-Pro-Arg-Rh110-D-Pro serves as a substrate for Factor XaI (FXIa) and exhibits binding affinity. This compound is composed of Rhodamine 110 linked to a peptide chain via a cleavable bond. Upon cleavage, the intensity of the fluorophore is enhanced. D-Leu-Pro-Arg-Rh110-D-Pro can be utilized to detect FXIa activity.

D-Leu-Pro-Arg-Rh110-D-Pro TFA is a substrate for Factor XaI (FXIa) known for its binding affinity. It consists of Rhodamine 110 linked to a peptide chain through a cleavable bond. The cleavage of this bond enhances the intensity of the fluorophore. D-Leu-Pro-Arg-Rh110-D-Pro TFA can be utilized to detect FXIa activity.