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

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

Cat. No.: HY-15759A
Handling Instructions

Napsagatran hydrate is a novel and specific thrombin inhibitor.

For research use only. We do not sell to patients.

Napsagatran hydrate Chemical Structure

Napsagatran hydrate Chemical Structure

CAS No. : 159668-20-9

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Description

Napsagatran hydrate is a novel and specific thrombin inhibitor.

IC50 & Target

Thrombin[1]

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].

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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.

References
Molecular Weight

576.67

Formula

C₂₆H₃₆N₆O₇S

CAS No.

159668-20-9

SMILES

O=C(NC[[email protected]]1CN(C(N)=N)CCC1)C[[email protected]@H](C(N(C2CC2)CC(O)=O)=O)NS(C3=CC4=CC=CC=C4C=C3)(=O)=O.O

Shipping

Room temperature in continental US; may vary elsewhere

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Napsagatran hydrate
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Napsagatran hydrate

Cat. No.: HY-15759A