2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. 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 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.

For research use only. We do not sell to patients.

FXIa-IN-9 Chemical Structure

FXIa-IN-9 Chemical Structure

CAS No. : 2816108-87-7

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Other Forms of FXIa-IN-9:

FXIa-IN-9 Related Antibodies

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Description

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].

IC50 & Target

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

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 value
equilibrium solubility (pH 1.2; pH 6.8) 81.0 μM; 171.6 μM
PPB % (mouse/rat/dog/human) 91.2/91.6/80.8/95.6
hERG inhibition (IC50) >10 μM
S9 aldehyde oxidase (AO) T1/2 > 180 min
hLM trapping assay no GSH and CN adducts
AMES genotoxicity test negative
in vitro micronucleus test negative

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

FXIa-IN-9 Related Antibodies
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].

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

Animal Model: Rabbit AV shunt thrombosis model[1]
Dosage: 1.7 mg/kg bolus + 2.0 mg/kg/h infusion, or 8.5 mg/kg bolus + 10 mg/kg/h infusion.
Administration: Intravenous dosing via the marginal ear vein 20 min prior to and 40 min during the AV shunt
Result: Showed 36.5% (1.7 mg/kg bolus + 2.0 mg/kg/h infusion) and 62.2% (8.5 mg/kg bolus + 10 mg/kg/h infusion) inhibitions in thrombus weight, respectively.
Animal Model: Rat, dog, monkey (pharmacokinetic assay)[1]
Dosage: 1 mpk, 2 mpk (i.v.); 5 mpk, 10 mpk (p.o.)
Administration: Intravenous injection, oral administration.
Result: Pharmacokinetic profile of FXIa-IN-9 in kinds of species.
animal species clearance (mL/min/kg) T1/2 (h) Vdss (L/kg) F% AUC (iv) (μM•h) AUC (po) (μM•h) Dose iv/po (mpk)
rat 10.7 1.4 0.8 36.4 5.5 10.0 2/10
dog 7.9 2.0 1.5 80.5 3.7 14.7 1/5
monkey 25.6 1.0 1.5 43.0 1.1 2.5 1/5
Molecular Weight

580.35

Formula

C23H18Cl2F3N9O2
CAS No.
SMILES

CN1N=NC=C1C2=CN(N=C2)C(CCOC(F)F)C3=CC=C(C=[N+]3[O-])C4=C(C=CC(Cl)=C4F)N5N=NC(Cl)=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FXIa-IN-9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FXIa-IN-92816108-87-7Factor XaFxaAntithromboticthrombosisanticoagulantplasma aPTTproteaseInhibitorinhibitorinhibit

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