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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- CAS No.: 292135-59-2
- Formule: C25H21ClF4N4O3S
- Masse moléculaire:568.97
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Animal Model:
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Dosage:0.08, 0.25, 0.82 and 2.5 mg/kg
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Administration:Intravenous injection (i.v.), for 90 min
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Result:Completely prevented thrombosis within 90 minutes when administered at a rate of 2.5 mg/kg/h intravenously.
Dose-dependent increased in the time of arterial patency with an EC₅₀ value (effective plasma concentration) of 137 nM.
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Animal Model:
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Dosage:1, 3 and 10 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Oral dose-dependent antithrombotic effect, with a significant result achieved at 10 mg/kg.
Chemical Information
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CAS No. 292135-59-2
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Masse moléculaire 568.97
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Formule C25H21ClF4N4O3S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DPC423 Related Classifications
HY-11090A Related Classifications
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