产品
编 号：F719506
分子式：C28H23Cl2F2N9O2
分子量：626.44
分子式：C28H23Cl2F2N9O2
分子量：626.44
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 1802425-99-5
产品详情
生物活性：
Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study.
体内研究：
Milvexian (20 mg/kg, 口服) 给药后 1 和 24 小时的平均血浆浓度分别为 2000 和 40 nM。Milvexian (0.8 mg/kg, 静脉注射) 给药后 10 分钟 和 8 小时的平均血浆浓度分别为 2000 和 100 nM。Milvexian (0.063-4 + 0.04- 2.68 mg/kg, 静脉滴注加持续输注) 可以抑制体内血栓形成。在兔中的药代动力学分析RouteDose (mg/kg)Clearance (mL/min/kg)Volume of Distribution (L/kgL)Half-life (h)Oral Bioavailability (%) i.v./p.o.0.8/206.71.42.514
Animal Model:The rabbit electrically mediated carotid arterial thrombosis model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Decreased carotid blood flow(CBF) to 32-76% and reduced thrombus weight by 15-70%. Decreased CBF to 40% of control initiated after 15 min. Decreased CBF to 39-66% after Seventy-five minutes.
Animal Model:The rabbit cuticle bleeding time model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Did not increase the carotid blood flow(BT) with combination of Aspirin (HY-14654).
Animal Model:The rabbit arteriovenous shunt model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)0.25?+?0.17, 1.0?+?0.67, and 4.0?+?2.68 ?mg/kg
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Reduced thrombus weight of thrombosis by 34.3?-66.9?%. Increased the prolongation of APTT with 1.54-3.12-fold, but did not alter the PT and TT.
体外研究：
Milvexian (约10 μM) 可增加人血浆中活化部分凝血活素时间，对人血浆中 ADP 、花生四烯酸和胶原蛋白对血小板聚集没有影响。
Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study.
体内研究：
Milvexian (20 mg/kg, 口服) 给药后 1 和 24 小时的平均血浆浓度分别为 2000 和 40 nM。Milvexian (0.8 mg/kg, 静脉注射) 给药后 10 分钟 和 8 小时的平均血浆浓度分别为 2000 和 100 nM。Milvexian (0.063-4 + 0.04- 2.68 mg/kg, 静脉滴注加持续输注) 可以抑制体内血栓形成。在兔中的药代动力学分析RouteDose (mg/kg)Clearance (mL/min/kg)Volume of Distribution (L/kgL)Half-life (h)Oral Bioavailability (%) i.v./p.o.0.8/206.71.42.514
Animal Model:The rabbit electrically mediated carotid arterial thrombosis model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Decreased carotid blood flow(CBF) to 32-76% and reduced thrombus weight by 15-70%. Decreased CBF to 40% of control initiated after 15 min. Decreased CBF to 39-66% after Seventy-five minutes.
Animal Model:The rabbit cuticle bleeding time model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Treatment: 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Did not increase the carotid blood flow(BT) with combination of Aspirin (HY-14654).
Animal Model:The rabbit arteriovenous shunt model
Dosage:Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)Prevention: 0.063 + 0.04, 0.25 + 0.17, and 1 + 0.67 (mg/kg + mg/kg/h)0.25?+?0.17, 1.0?+?0.67, and 4.0?+?2.68 ?mg/kg
Administration:Intravenous injection (i.v.) plus a continuous infusion
Result:Reduced thrombus weight of thrombosis by 34.3?-66.9?%. Increased the prolongation of APTT with 1.54-3.12-fold, but did not alter the PT and TT.
体外研究：
Milvexian (约10 μM) 可增加人血浆中活化部分凝血活素时间，对人血浆中 ADP 、花生四烯酸和胶原蛋白对血小板聚集没有影响。
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