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DS-1040 Tosylate

CAS No. : 1335138-89-0

产品活性：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.

研究领域：Others

作用靶点：Others

In Vitro: DS-1040 Tosylate inhibits 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 ED_max 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 EC_max values are 114 and 231 nmol/L, respectively.

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