FXIa-IN-16
FXIa-IN-16 is an orally active selective FXIa inhibitor with an IC50 of 0.19 nM. FXIa-IN-16 exerts highly selective competitive inhibition on endogenous FXIa, blocks the thrombin amplification loop to inhibit thrombosis, while preserving exogenous physiological hemostatic function. FXIa-IN-16 can be used in thrombosis-related research.
For research use only. We do not sell to patients.
- CAS No.: 3046390-69-3
- Formula: C24H18ClFN8O2
- Molecular Weight:504.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
FXIa-IN-16 (Compound 43) (30 min) potently inhibits purified human FXIa, with an IC50 of 0.19 nM[1].
FXIa-IN-16 (3 nM-1.3 μM; 3 min) concentration-dependently prolongs the activated partial thromboplastin time (aPTT) in human plasma, with an EC1.5x of 0.43 μM, and exerts no significant effect on the extrinsic coagulation pathway (PT)[1].
FXIa-IN-16 (0.3-13.3 μM; 3 min) concentration-dependently prolongs the activated partial thromboplastin time (aPTT) of mouse plasma, with an EC1.5x of 1.6 μM[1].
FXIa-IN-16 (30 min) exhibits high selectivity for human FXIa, with a selectivity of over 1000-fold against 7 other serine proteases, and a selectivity index of 1168 relative to plasma kallikrein[1].
FXIa-IN-16 (1 μM-50 μM; 24 h) exhibits no significant cytotoxicity against AC16, HK-2 and HepG2 cells[1].
FXIa-IN-16 (1 μM-50 nM) potently inhibits the catalytic hydrolysis of substrates by FXIa in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AC16, HK-2, and HepG2 cells
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Concentration:1 μM, 10 μM, 50 μM
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Incubation Time:24 h
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Result:Demonstrated no significant cytotoxicity.
FXIa-IN-16 (2 mg/kg or 6 mg/kg; i.v.; single administration; 30 min) exhibits significant antithrombotic activity in FeCl3-induced rabbit arterial thrombosis models, and dose-dependently reduces the weights of wet and dry thrombi significantly[1].
FXIa-IN-16 (30 mg/kg or 60 mg/kg; i.g.; single dose; tail amputation performed 30 min post-administration) exhibits extremely low bleeding risk in the mouse tail bleeding model and does not significantly prolong bleeding time[1].
FXIa-IN-16 (2 mg/kg or 6 mg/kg; i.v.; single administration; incision made 30 min post-administration) exerts a minimal bleeding risk effect in the rabbit ear bleeding model and does not significantly prolong bleeding time[1].
FXIa-IN-16 (60 mg/kg or 100 mg/kg; i.g.; single administration; 14 days) exhibits excellent in vivo safety in a mouse acute toxicity model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FeCl3-induced C57BL/6J mouse arterial thrombosis model (exposed common carotid artery wrapped with 7.5% FeCl3 filter paper for 3 min)[1]
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Dosage:5 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:i.g.; single dose; tested at 0.5, 2, and 4 h
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Result:Significantly increased the peak and mean blood flow velocities in the carotid artery in a dose-dependent manner.
The peak and mean blood flow velocities remained significantly elevated at 2 and 4 hours after administration, demonstrating a durable antithrombotic effect.
The in vivo antithrombotic activity positively correlated with the inhibition level of FXIa activity in the plasma.
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Animal Model:FeCl3-induced male New Zealand white rabbit arterial thrombosis model (20% FeCl3 filter paper applied to the exposed carotid artery for 5 min)[1]
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Dosage:2 mg/kg, 6 mg/kg
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Administration:i.v.; single dose; evaluated 30 min after administration
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Result:Significantly reduced both wet and dry thrombus weights in a dose-dependent manner.
Achieved a reduction of more than 50% in both wet and dry thrombus weights at the 2 mg/kg dose.
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Animal Model:C57BL/6J mouse tail bleeding model (amputation of the distal 5-mm segment of the tail)[1]
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Dosage:30 mg/kg, 60 mg/kg
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Administration:i.g.; single dose; tail amputated 30 min after administration
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Result:Did not significantly extend the time to bleeding cessation compared to the control group, indicating a very low bleeding risk in vivo.
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Animal Model:Male New Zealand white rabbit ear bleeding model (4 mm long and 1 mm deep skin incision made parallel to the external vein of the ear)[1]
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Dosage:2 mg/kg, 6 mg/kg
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Administration:i.v.; single dose; incision made 30 min after administration
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Result:Showed minimal bleeding effects and did not significantly increase the bleeding time.
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Animal Model:C57BL/6J mouse acute toxicity model (healthy mice kept under normal conditions)[1]
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Dosage:60 mg/kg, 100 mg/kg
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Administration:i.g.; single dose; continuously monitored for 14 days
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Result:Did not induce any death, anaphylactic responses, or abnormal behavior during the 14-day monitoring period.
Body weights increased normally without significant weight loss.
No obvious toxicity or pathological damage was observed in the hematoxylin and eosin (H&E) stained tissue sections of the liver, heart, kidney, lung, and spleen.
The serum levels of aspartate aminotransferase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP) did not show abnormal changes.
Chemical Information
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CAS No. 3046390-69-3
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Molecular Weight 504.90
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Formula C24H18ClFN8O2
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SMILES
O=C1N(CC2=NC=CC(C3=C(F)N=C(N)C=C3)=C2)C=C(OC)C(C4=CC(Cl)=CC=C4N5C=NN=N5)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FXIa-IN-16 Related Classifications
HY-172400 Related Classifications
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