2. Metabolic Enzyme/Protease
  3. Thrombin
  4. Napsagatran hydrate

Napsagatran hydrate  (Synonyms: Ro 46-6240 hydrate; Ro 46-6240/010 hydrate)

目录号: HY-15759A
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摩尔计算器

Napsagatran hydrate 是一种新型的特异性凝血酶 (thrombin) 抑制剂。

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Napsagatran hydrate Chemical Structure

Napsagatran hydrate Chemical Structure

CAS No. : 159668-20-9

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Other Forms of Napsagatran hydrate:

Napsagatran hydrate 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Napsagatran hydrate is a novel and specific thrombin inhibitor.

IC50 & Target

Thrombin[1]
体外研究
(In Vitro)

Napsagatran (Ro 46-6240), the selective thrombin inhibitor, induces a dose-dependent prolongation of the activated partial thromboplastin time (aPTT) and prothrombin time (PT) that is evident 15 min after administration of the bolus of Napsagatran. Napsagatran also reduces the time to reperfusion in a dose-dependent manner and delays or prevents reocclusion[1]. The decreasing intracellular amount and efflux of compound from the cells into the medium is measured. The measured CLint,efflux values are 0.13±0.06, 3.2±0.6, 10.1±2.3, and 110±2.8 for Digoxin, Fexofenadine, Napsagatran, and Rosuvastatin, respectively, thus representing drugs with a >800-fold range of efflux rates[2].

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

Napsagatran hydrate 相关抗体:
体内研究
(In Vivo)

After the first hour of drug administration (from 0 to 60 min), the incorporated radioactivity into thrombi increased from baseline by 73±13, 67±22 and 32±10% in placebo, AP-1 and Napsagatran-treated rabbits, respectively. Statistical analysis confirm that thrombus growth in the placebo and AP-1 treated rabbits is not different. In contrast, reduction of 125I-fibrinogen incorporation by Napsagatran is statistical different from the placebo group (P<0.01)[3].

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

576.67

Formula

C26H36N6O7S
CAS 号
中文名称

奈沙加群水合物
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
Kinase Assay
[2]

Hepatocytes in 12-well plates are preloaded until a maximal intracellular concentration is reached. Measuring the compound efflux at maximal intracellular concentration gives the efflux at steady state. Preload times and compound concentrations are decided from measured uptake data in pilot experiments (Digoxin, 10 μM for 15 minutes; Fexofenadine, 1 μM for 30 minutes; Napsagatran, 10 μM for 30 minutes; and Rosuvastatin, 1 μM for 15 minutes). After preloading, the wells are washed three times in 37°C Krebs-Henseleit buffer with 10 mM HEPES (GIBCO) pH 7.4 (KHL) to ensure that the wells are free from remaining compound. Efflux experiments are started by adding 300 μL KHL (37°C) to each well. Cells are also lysed immediately after washing to determine the initial intracellular concentrations at the start of the experiment. The contribution of ABC-efflux transporter activity to the measured efflux is assayed using 0.5 μM of the inhibitors Elacridar and Fumitremorgin C (FTC)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Rabbits[3]
The experiment is initiated by a bolus injection followed by infusion of 125I-human fibrinogen. Increase of tracer uptake within 30 min infusion of more than 30% of background value is indicative of onset of thrombus growth and thus, the counts are set to zero and Rabbits receive either Napsagatran a specific thrombin inhibitor (10 µg/kg per min in continuous i.v. infusion) or repetitive i.v. bolus of the monoclonal antiRabbits TF antibody AP-1 (600 µg/kg) at hourly intervals. The placebo-treated Rabbits (control group) receive either saline infused at 1 mL/kg or four boli of an irrelevant IgG Rabbits mAb.

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

Napsagatran hydrate 相关分类

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Keywords:

Napsagatran159668-20-9Ro 46-6240Ro 46-6240/010奈沙加群水合物ThrombinInhibitorinhibitorinhibit

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