产品
编 号：F755199
分子式：C31H29ClN8O5
分子量：629.07
分子式：C31H29ClN8O5
分子量：629.07
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CAS No: 2744293-04-5
产品详情
生物活性：
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>.
体内研究：
FXIa-IN-8 shows selectivity for FXIa and PKal with IC50s of 14.2, 27900 nM, respectively.FXIa-IN-8 (6.5, 19.5 mg/kg; i.v.) shows antithrombotic activity in vivo.FXIa-IN-8 (50, 100 mg/kg; i.v.) shows no acute toxicity.FXIa-IN-8 (10 mg/kg; i.v.) shows moderate PK profiles.FXIa-IN-8 (19.5, 39 mg/kg) exhibits a much lower bleeding risk than heparin sodium at 300 IU/kg.Pharmacokinetic Parameters of FXIa-IN-8 in Male SD rats.compd 35T1/2 (h) Cmax (μg/mL)AUC0-t (h·μg/mL) AUC0-∞ (h·μg/mL) Vz(mL/kg) Cl (mL/h/kg)MRT0-t (h)
i.v. (10 mg/kg)1.265718.318.49695530.32
Male SD rats; 10 mg/kg for i.v..Animal Model:Male SD rats
Dosage:10 mg/kg (300 IU/kg (2.7 mg/kg) heparin sodium were injected into the tail vein 10 min before surgery)
Administration:I.v.
Result:Showed moderate PK profiles with a half-life value (T1/2) of 1.26 h and a clearance (Cl) value of 553 mL/h/kg.
Animal Model:C57BL/6J mice (FeCl3-induced carotid artery thrombus model)
Dosage:6.5, 19.5 mg/kg
Administration:I.v.
Result:Slightly prolonged the time of occlusion at 6.5 mg/kg, and showed excellent antithrombotic activity at 35 mg/kg.
Animal Model:ICR mice
Dosage:50, 100 mg/kg
Administration:I.v.
Result:Showed no obvious toxic reaction to different tissues of mice.
Animal Model:C57BL/6J mice
Dosage:19.5, 39, 20, 60, 100 mg/kg
Administration:I.v.
Result:Showed a low bleeding risk at 60 and 100 mg/kg.
体外研究：
FXIa-IN-8 (compound 35) (0-250 μg/mL) shows significant anticoagulant activity toward the intrinsic pathway without affecting the extrinsic pathway.
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>.
体内研究：
FXIa-IN-8 shows selectivity for FXIa and PKal with IC50s of 14.2, 27900 nM, respectively.FXIa-IN-8 (6.5, 19.5 mg/kg; i.v.) shows antithrombotic activity in vivo.FXIa-IN-8 (50, 100 mg/kg; i.v.) shows no acute toxicity.FXIa-IN-8 (10 mg/kg; i.v.) shows moderate PK profiles.FXIa-IN-8 (19.5, 39 mg/kg) exhibits a much lower bleeding risk than heparin sodium at 300 IU/kg.Pharmacokinetic Parameters of FXIa-IN-8 in Male SD rats.compd 35T1/2 (h) Cmax (μg/mL)AUC0-t (h·μg/mL) AUC0-∞ (h·μg/mL) Vz(mL/kg) Cl (mL/h/kg)MRT0-t (h)
i.v. (10 mg/kg)1.265718.318.49695530.32
Male SD rats; 10 mg/kg for i.v..Animal Model:Male SD rats
Dosage:10 mg/kg (300 IU/kg (2.7 mg/kg) heparin sodium were injected into the tail vein 10 min before surgery)
Administration:I.v.
Result:Showed moderate PK profiles with a half-life value (T1/2) of 1.26 h and a clearance (Cl) value of 553 mL/h/kg.
Animal Model:C57BL/6J mice (FeCl3-induced carotid artery thrombus model)
Dosage:6.5, 19.5 mg/kg
Administration:I.v.
Result:Slightly prolonged the time of occlusion at 6.5 mg/kg, and showed excellent antithrombotic activity at 35 mg/kg.
Animal Model:ICR mice
Dosage:50, 100 mg/kg
Administration:I.v.
Result:Showed no obvious toxic reaction to different tissues of mice.
Animal Model:C57BL/6J mice
Dosage:19.5, 39, 20, 60, 100 mg/kg
Administration:I.v.
Result:Showed a low bleeding risk at 60 and 100 mg/kg.
体外研究：
FXIa-IN-8 (compound 35) (0-250 μg/mL) shows significant anticoagulant activity toward the intrinsic pathway without affecting the extrinsic pathway.
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