2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. FXIa-IN-10

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability.

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FXIa-IN-10

FXIa-IN-10 Estructura química

No. CAS : 2816108-08-2

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Descripciòn

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability[1].

IC50 & Target

Ki: 0.17 nM (FXIa)[1]
In Vivo

FXIa-IN-10 (Compound 3f) (1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg; i.v.; twice) shows antithrombotic efficacy in a rabbit AV shunt thrombosis model[1].
FXIa-IN-10 (0-10 mg/kg; p.o.; once) demonstrates oral bioavailability in preclinical species (rat 36.4%, dog 80.5%, and monkey 43.0%)[1].

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

Animal Model: Male New Zealand White (NZW) rabbits, AV shunt thrombosis model[1]
Dosage: 1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg
Administration: Intravenous injection, 20 min prior to and 40 min during the AV shunt
Result: Reduced thrombus weights in a dose-dependent manner.
Animal Model: Sprague-Dawley rats, Beagle dogs, Cynomolgus monkeys[1]
Dosage: 1, 2, 5 or 10 mg/kg
Administration: Intravenous or oral administration (Pharmacokinetic Analysis)
Result: Pharmacokinetic Profile of FXIa-IN-10 (Compound 3f) in Preclinical Speciesa[1]
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 ± 1.8 1.4 ± 0.0 0.8 ± 0.1 36.4 5.5 ± 1.0 10.0 ± 2.4 2/10
monkey 25.6 ± 4.0 1.0 ± 0.4 1.5 ± 0.4 43.0 1.1 ± 0.2 2.5 ± 0.3 1/5

aCompound was dosed as a free base, vehicle for iv: 20% HPbCD and po: 10% ethanol; 70% PEG-400; 20% water. Data were derived from three animals per study.
Peso molecular

580.35

Fòrmula

C23H18Cl2F3N9O2
No. CAS
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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FXIa-IN-10 Related Classifications

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Keywords:

FXIa-IN-102816108-08-2Factor XaFxaactivated factor XIFXIagood oral bioavailabilityantithrombotic efficacyInhibitorinhibitorinhibit

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Nombre del producto:
FXIa-IN-10
Cat. No.:
HY-151196
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