FXIa-IN-9_product_DataBase

Bioactivity	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 Ki: 0.17 nM, rabbit FXIa Ki: 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].
Target	Ki: 0.17 nM (human FXIa), 0.5 nM (rabbit FXIa).
Invitro	FXIa-IN-9 has anticoagulant activity, with EC1.5x 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].property/assay
In Vivo	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]. Animal Model:
Name	FXIa-IN-9
CAS	2816108-87-7
Formula	C23H18Cl2F3N9O2
Molar Mass	580.35
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB

FXIa-IN-9

CAS: 2816108-87-7 F: C23H18Cl2F3N9O2 W: 580.35