FXIa-IN-9 

FXIa-IN-9 (compound 3f) is a potent and selective FXIa inhibitor. FXIa-IN-9 can bind with FXIa and form hydrogen bond (human FXIa K_i: 0.17 nM, rabbit FXIa K_i: 0.5 nM). FXIa-IN-9 also has anticoagulant activity, and can be used in the research of thromboembolic diseases such as atrial fibrillation, stroke, myocardial infarction, deep vein thrombosis, and pulmonary embolism^[1].

Ki: 0.17 nM (human FXIa), 0.5 nM (rabbit FXIa)^[1].

FXIa-IN-9 has anticoagulant activity, with EC_1.5x values of 1.31 μM (human plasma aPTT) and 1.39 μM (rabbit plasma aPTT), respectively^[1].
FXIa-IN-9 (10 μM, 5-15 min) is highly selective for FXIa against other human serine protease, except for plasma kallikrein (IC₅₀: 0.023 μM)^[1].
FXIa-IN-9 shows the plasma protein binding ranges from 80.8 to 95.6%, and pharmacological profile is as follows^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FXIa-IN-9 (marginal ear intravenous injection, 1.7-10 mg/kg, dosing at 20 min prior to and 40 min during the AV shunt) achieves more than 50% thrombus reduction in the rabbit arteriovenous (AV) shunt thrombosis model^[1].
FXIa-IN-9 (i.v. or p.o., 1-10 mpk ) shows low clearance in rat and dog and moderate clearance in the monkey as well as good oral bioavailability^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

580.35

C₂₃H₁₈Cl₂F₃N₉O₂

2816108-87-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Guozhang Xu, et al. Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions. J Med Chem. 2022 Jul 21.  [Content Brief]