DPC423 

DPC423 is a selective and orally active factor Xa inhibitor with a K_is of 0.15 (human) and 0.3 (rabbit) nM. DPC423 exhibits K_is of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 has demonstrated antithrombotic effects in animal models, and when used in combination with Aspirin (HY-14654), it shows a strong synergistic effect. DPC423 can be used for the study of anticoagulation of arterial thrombosis^[1][2].

DPC423 (0.08-2.5 mg/kg, i.v., for 90 min) increases blood flow in the carotid artery with an ED₅₀ of 0.6 mg/kg^[1][2].
DPC423 (1-10 mg/kg, p.o., single dose) exhibits a dose-dependent anti-thrombotic effect^[1][2].

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

568.97

C₂₅H₂₁ClF₄N₄O₃S

292135-59-2

NCC1=CC(N2C(C(NC3=CC=C(C4=CC=CC=C4S(=O)(C)=O)C=C3F)=O)=CC(C(F)(F)F)=N2)=CC=C1.Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. D J Pinto, et al. Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa. J Med Chem. 2001 Feb 15;44(4):566-78.  [Content Brief]

  [2]. Wong PC, et al. Nonpeptide factor Xa inhibitors III: effects of DPC423, an orally-active pyrazole antithrombotic agent, on arterial thrombosis in rabbits. J Pharmacol Exp Ther. 2002 Dec;303(3):993-1000.  [Content Brief]