2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Factor Xa Kallikrein Thrombin Ser/Thr Protease
  4. DPC423

DPC423 是一种具有选择性和口服活性的 factor Xa 抑制剂，其对人源和兔源的 Ki 值分别为 0.15 nM 和 0.3 nM。DPC423 对人源胰蛋白酶 (trypsin)、血浆激肽释放酶 (plasma kallikrein) 和凝血酶 (thrombin) 的 Ki 值分别为 60 nM、61 nM 和 6000 nM。DPC423 可阻断凝血酶原酶复合物的形成，减少凝血酶的生成，抑制纤维蛋白的形成和血小板活化。DPC423 在动物模型中具有抗血栓作用，并且与 Aspirin (HY-14654) 联合使用时，显示出强协同作用。DPC423 可用于动脉血栓的抗凝研究。

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DPC423

DPC423 Chemical Structure

CAS No. : 292135-59-2

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DPC423 相关抗体

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KLK1 KLK5 KLK8 KLK14 KLKB1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 has demonstrated antithrombotic effects in animal models, and when used in combination with Aspirin (HY-14654), it shows a strong synergistic effect. DPC423 can be used for the study of anticoagulation of arterial thrombosis[1][2].

体内研究
(In Vivo)

DPC423 (0.08-2.5 mg/kg，静脉注射，持续 90 分钟) 可增加颈动脉血流量，其 ED50 为 0.6 mg/kg[1][2]。
DPC423 (1-10 mg/kg，口服，单次给药) 表现出剂量依赖性的抗血栓作用[1][2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Carotid artery electrical injury thrombosis model (ECAT) established in male New Zealand white rabbits[1][2]
Dosage: 0.08, 0.25, 0.82 and 2.5 mg/kg
Administration: Intravenous injection (i.v.), for 90 min
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.
Animal Model: Carotid artery electrical injury thrombosis model (ECAT) established in male New Zealand white rabbits[1][2]
Dosage: 1, 3 and 10 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Oral dose-dependent antithrombotic effect, with a significant result achieved at 10 mg/kg.
分子量

568.97

Formula

C25H21ClF4N4O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DPC423 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DPC423292135-59-2DPC 423DPC-423Factor XaKallikreinThrombinSer/Thr ProteaseFxaKLKKallikrein-related peptidaseSerine proteasesSerine endopeptidasesThreonine proteasesfXafactor XaECATelectric current-induced arterial thrombosisAPTTInhibitorinhibitorinhibit

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目录号：
HY-11090A
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