DPC423 (free base)

DPC423 free base is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits Kis of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis[1][2].

Product Specifications

CAS Number

[209957-47-1]

UNSPSC

12352005

Target

Factor Xa; Kallikrein; Ser/Thr Protease; Thrombin

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

O=C(C1=CC(C(F)(F)F)=NN1C2=CC=CC(CN)=C2)NC3=CC=C(C4=CC=CC=C4S(=O)(C)=O)C=C3F

Molecular Formula

C25H20F4N4O3S

Molecular Weight

532.51

References & Citations

[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. |[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.