| Identification | Back Directory | [Name]
DS-1040 (Tosylate) | [CAS]
1335138-89-0 | [Synonyms]
DS-1040 (Tosylate)
DS-1040 tosylate
(DS 1040
DS 1040 Tosylate,DS1040 Tosylate | [Molecular Formula]
C23H35N3O5S | [MDL Number]
MFCD31544337 | [MOL File]
1335138-89-0.mol | [Molecular Weight]
465.61 |
| Hazard Information | Back Directory | [Description]
DS-1040 Tosylate is an inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa), used for the treatment of acute ischemic stroke (AIS). | [Uses]
DS-1040 Tosylate 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 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[1].
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[1].
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[1].
| Animal Model: | Male Slc:Wistar rats[1] | | Dosage: | 0.0005, 0.005, 0.05, 0.5 mg/kg | | Administration: | IV | | Result: | Significantly reduced the microthrombi index at doses of 0.005 mg/kg and greater.
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| [References]
[1]. Zhou J, et al. A first-in-human study of DS-1040, an inhibitor of the activated form of thrombin-activatable fibrinolysis inhibitor, in healthy subjects. J Thromb Haemost. 2017 May;15(5):961-971. |
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