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.
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- No. CAS: 209957-47-1
- Fòrmula: C25H20F4N4O3S
- Peso molecular:532.51
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
DPC423 free base (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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No. CAS 209957-47-1
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Peso molecular 532.51
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Fòrmula C25H20F4N4O3S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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 free base Related Classifications
HY-11090 Related Classifications
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