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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 209957-47-1
- 分子式: C25H20F4N4O3S
- 分子量:532.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 209957-47-1
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分子量 532.51
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DPC423 free base 関連分類
HY-11090 関連分類
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