FXIa-IN-8-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE FXIa-IN-8 Cat. No.: HY-144658 CAS No.: 2744293-04-5 分⼦式: C₃₁H₂₉ClN₈O₅ 分⼦量: 629.07 作⽤靶点: Factor Xa 作⽤通路: Metabolic Enzyme/Protease 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 FXIa-IN-8 是⼀种有效的选择性 FXIa 抑制剂， IC50 为 14.2 nM。FXIa-IN-8 具有抗⾎栓形成活性，且不会增加 出⾎风险和明显的毒性sup[1]。 IC50 Target IC50: 14.2 nM (FXIa); 27900 nM (PKal) [1] 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 [1]. 体内研究 FXIa-IN-8 shows selectivity for FXIa and PKal with IC50s of 14.2, 27900 nM, respectively [1]. FXIa-IN-8 (6.5, 19.5 mg/kg; i.v.) shows antithrombotic activity in vivo [1]. FXIa-IN-8 (50, 100 mg/kg; i.v.) shows no acute toxicity [1]. FXIa-IN-8 (10 mg/kg; i.v.) shows moderate PK profiles [1].FXIa-IN-8 (19.5, 39 mg/kg) exhibits a much lower bleeding risk than heparin sodium at 300 IU/kg [1]. Pharmacokinetic Parameters of FXIa-IN-8 in Male SD rats [1]. compd 35 T1/2 (h) Cmax (µg/mL) AUC0-t (h·µg/mL) AUC0-∞ (h·µg/mL) Vz(mL/kg) Cl (mL/h/kg) MRT0-t