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 inhibits proliferation of vascular smooth muscle cells in cell culture systems. DX-9065a inactivates both free and fibrin-bound FXa. DX-9065a effectively affects the clot-associated procoagulant activity^[1].

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

After i.v. injection to rabbits, DX-9065a displays prolonged anti-factor Xa activity and inhibition of thrombin generation^[1].
After p.o. administration, DX-9065a causes a reduction in tissue factor-induced mortality of mice with ED₅₀ value of 56 mg/kg^[1].
When given i.v. to rats, DX-9065a exhibits a dose-dependent antithrombotic effect against factor Xa + stasis-induced venous thrombosis (ED₅₀ = 1.2 mg/kg i.v.), but also in an arteriovenous shunt thrombosis model (ED₅₀ = 8.1 mg/kg i.v.) without affecting bleeding time significantly. Similar effects were obtained after s.c. or p.o. administration^[1].
In rabbits, after i.v., s.c. or p.o. administration, DX-9065a inhibits stasis-induced thrombosis after injection of tissue factor with ED₅₀ values of 0.03 mg/kg, 0.3 mg/kg and 50.5 mg/kg, respectively. DX-9065a inhibits in a dose-dependent manner endotoxin-induced venous thrombosis in the rabbit (ED₅₀ = 0.25 mg/kg i.v.) and reduces the decrease in platelet number and circulating fibrinogen levels in an experimental model of tissue factor-induced disseminated intravascular coagulation^[1].

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

571.06

C₂₆H₃₉ClN₄O₈

155204-81-2

N=C(N)C1=CC=C2C(C=C(C[C@H](C(O)=O)C3=CC=C(O[C@@H]4CN(C(C)=N)CC4)C=C3)C=C2)=C1.O.O.O.O.O.Cl

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]