Napsagatran hydrate is a novel and specific thrombin inhibitor.

Product information

CAS Number: 159668-20-9

Molecular Weight: 576.67

Formula: C26H36N6O7S

Chemical Name: 2-[(2S)-3-({[(3S)-1-carbamimidoylpiperidin-3-yl]methyl}carbamoyl)-N-cyclopropyl-2-(naphthalene-2-sulfonamido)propanamido]acetic acid hydrate

Smiles: O.NC(=N)N1C[C@H](CNC(=O)C[C@H](NS(=O)(=O)C2=CC3=CC=CC=C3C=C2)C(=O)N(CC(O)=O)C2CC2)CCC1

InChiKey: TYAMPCPJIDBUQW-ZLLYMXMVSA-N

InChi: InChI=1S/C26H34N6O6S.H2O/c27-26(28)31-11-3-4-17(15-31)14-29-23(33)13-22(25(36)32(16-24(34)35)20-8-9-20)30-39(37,38)21-10-7-18-5-1-2-6-19(18)12-21;/h1-2,5-7,10,12,17,20,22,30H,3-4,8-9,11,13-16H2,(H3,27,28)(H,29,33)(H,34,35);1H2/t17-,22-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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).

Products are for research use only. Not for human use.