产品
编 号：F756129
分子式：C23H18Cl2F3N9O2
分子量：580.35
分子式：C23H18Cl2F3N9O2
分子量：580.35
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CAS No: 2816108-08-2
产品详情
生物活性：
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.
体内研究：
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.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%).Animal Model:Male New Zealand White (NZW) rabbits, AV shunt thrombosis model
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
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 Speciesaanimal speciesclearance (mL/min/kg) T1/2 (h) Vdss (L/kg) F% AUC (iv) (μM?h) AUC (po) (μM?h) Dose iv/po (mpk)
rat10.7 ± 1.81.4 ± 0.00.8 ± 0.136.45.5 ± 1.010.0 ± 2.42/10
monkey25.6 ± 4.01.0 ± 0.41.5 ± 0.443.01.1 ± 0.22.5 ± 0.31/5
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.
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.
体内研究：
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.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%).Animal Model:Male New Zealand White (NZW) rabbits, AV shunt thrombosis model
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
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 Speciesaanimal speciesclearance (mL/min/kg) T1/2 (h) Vdss (L/kg) F% AUC (iv) (μM?h) AUC (po) (μM?h) Dose iv/po (mpk)
rat10.7 ± 1.81.4 ± 0.00.8 ± 0.136.45.5 ± 1.010.0 ± 2.42/10
monkey25.6 ± 4.01.0 ± 0.41.5 ± 0.443.01.1 ± 0.22.5 ± 0.31/5
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.
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