DS-1040 (Tosylate)
- Product Name
- DS-1040 (Tosylate)
- CAS No.
- 1335138-89-0
- Chemical Name
- DS-1040 (Tosylate)
- Synonyms
- DS-1040 (Tosylate);DS-1040 tosylate (DS 1040;DS 1040 Tosylate,DS1040 Tosylate
- CBNumber
- CB73356149
- Molecular Formula
- C23H35N3O5S
- Formula Weight
- 465.61
- MOL File
- 1335138-89-0.mol
DS-1040 (Tosylate) Property
- storage temp.
- Store at -20°C
- form
- Solid
- color
- White to off-white
- Water Solubility
- Water: 100 mg/mL (214.77 mM)
DS-1040 (Tosylate) Chemical Properties,Usage,Production
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. |
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.
DS-1040 (Tosylate) Preparation Products And Raw materials
Raw materials
Preparation Products
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