| Description | DS-1040 Tosylate is an oral active, selective thrombolytic inhibitor with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa, is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases[1]. |
| In vitro | Ds-1040 Tosylate inhibited human carboxypeptidase N (CPN) in vitro with an IC50 of 3.02 mM. |
| In vivo | DS-1040 Tosylate (0.0005-0.5 mg/kg; IV) significantly reduces the microthrombi index at doses of 0.005 mg/kg and greater. DS1040 (0.016, 0.031, 0.063, 0.13, 0.25, 0.50 mg/kg; i.v.) increases plasma D-dimer levels in a dose-dependent manner in the microthrombosis model. ED50 and EDmax are 122 and 221 nmol/L, respectively. DS-1040 (0.25, 0.5, 1, 2, 4, 8, 16 mg/kg; orally) also increases plasma D-dimer levels. EC50 and ECmax values are 114 and 231 nmol/L, respectively. |
| Target activity | TAFIa (rat):8.01 nM , TAFIa (human):5.92 nM |
| molecular weight | 465.61 |
| Molecular formula | C23H35N3O5S |
| CAS | 1335138-89-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 100 mg/mL (214.77 mM), Sonication is recommended. |
| References | 1. Noguchi K, et al. Fibrinolytic potential of DS-1040, a novel orally available inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa). Thromb Res. 2018 Aug;168:96-101. |