DX-9065a 

DX-9065a is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a K_i of 41 nM for human FXa. DX-9065a has low activity against other serine proteases. DX-9065a has strong anticoagulant actions^[1][2].

DX-9065a 可抑制细胞培养系统中血管平滑肌细胞的增殖。DX-9065a 可灭活游离和纤维蛋白结合的 FXa。DX-9065a 可有效影响血凝块相关的促凝活性^[1]。

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

静脉注射后注射给兔子后，DX-9065a 显示出延长的抗 Xa 因子活性和抑制凝血酶生成^[1]。
口服给药后，DX-9065a 可降低小鼠组织因子诱导的死亡率，ED₅₀ 值为 56 mg/kg^[1]。
给大鼠静脉注射时，DX-9065a 对 Xa 因子 + 瘀滞诱导的静脉血栓形成 (ED₅₀ = 1.2 mg/kg 静脉注射) 表现出剂量依赖性的抗血栓作用，但在动静脉分流血栓形成模型 (ED₅₀ = 8.1 mg/kg 静脉注射) 中也表现出抗血栓作用，且不会显着影响出血时间。皮下或口服给药后也获得了类似的效果^[1]。
在兔子中，静脉、皮下或口服给药后，DX-9065a 可抑制注射组织因子后瘀滞诱发的血栓形成，ED₅₀ 值分别为 0.03 mg/kg、0.3 mg/kg 和 50.5 mg/kg。DX-9065a 以剂量依赖性方式抑制兔子内毒素诱发的静脉血栓形成（ED₅₀ = 0.25 mg/kg 静脉注射），并减少组织因子诱发的弥漫性血管内凝血实验模型中血小板数量和循环纤维蛋白原水平的下降^[1]。

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

571.06

C₂₆H₃₉ClN₄O₈

155204-81-2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Brigitte Kaiser. DX-9065a, a direct inhibitor of factor Xa. Cardiovasc Drug Rev. 2003 Summer;21(2):91-104.  [Content Brief]

  [2]. J M Herbert, et al. DX 9065A a novel, synthetic, selective and orally active inhibitor of factor Xa: in vitro and in vivo studies. J Pharmacol Exp Ther. 1996 Mar;276(3):1030-8.  [Content Brief]