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

Napsagatran hydrate is a novel and specific thrombin inhibitor.

Thrombin^[1]

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 CL_int,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].

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

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].

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

576.67

C₂₆H₃₆N₆O₇S

159668-20-9

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. Pratico D, et al. Interaction of a thrombin inhibitor and a platelet GP IIb/IIIa antagonist in vivo: evidence thatthrombin mediates platelet aggregation and subsequent thromboxane A2 formation during coronary thrombolysis. J Pharmacol Exp Ther. 1997 Jun;2  [Content Brief]

  [2]. Lundquist P, et al. Prediction of in vivo rat biliary drug clearance from an in vitro hepatocyte efflux model. Drug Metab Dispos. 2014 Mar;42(3):459-68.  [Content Brief]

  [3]. Himber J, et al. Inhibition of tissue factor limits the growth of venous thrombus in the rabbit. J Thromb Haemost. 2003 May;1(5):889-95.  [Content Brief]