292135-59-2
Chemical Structure
DPC423
- CAS. Nr.: 292135-59-2
- Formula:C25H21ClF4N4O3S
- Molecular Weight:568.97
IUPAC Name: 1-(3-(aminomethyl)phenyl)-N-(3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide hydrochloride
InChIKey: LJBVKRYJJZQKGE-UHFFFAOYSA-N
SMILES: 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
Biological Activity: DPC423 is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 exhibits Kis 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 can be used for the study of anticoagulation of arterial thrombosis[1][2].
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DPC423 | DPC423 is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 exhibits Kis 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 can be used for the study of anticoagulation of arterial thrombosis. | |||||||||||||||||||||
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References
- [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]
